Central Nervous System Agents in Medicinal Chemistry, 2022
Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics med... more Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics medicines presently available. This resistance now poses a significant challenge to researchers to beat malaria parasitic infections. Strategies such as investigating newer hybrid chemical entities and specified drug targets may help us spot new efficient derivatives that bind to the parasites in a more specific manner and inhibit their growth. Objective: To scientifically perform the experimental, pharmacological, and computational studies of pyrazole-based furanone hybrids as novel antimalarial agents. Methods: A series of new furanone-based pyrazole derivatives were synthesized and investigated as potential antimalarial agents by performing in vitro antimalarial activity. To get further optimization, these synthesized derivatives were virtually screened based on ADME-T filters, and molecular docking studies were also accomplished on the crystal structures of Plasmodium falciparum lactate...
Summary The objective of this study was to formulate and evaluate Salbutamol sulphate matrix tabl... more Summary The objective of this study was to formulate and evaluate Salbutamol sulphate matrix tablets, sustained release dosage form, for the treatment of Chronic Obstructive Pulmonary Disease (COPD). The matrix tablets were prepared by direct comression method using two polymers such as hydroxyl propyl methyl cellulose (HPMC) and xanthan gum in varying ratios. Tablets blends were evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. The compressed tablets were then evaluated for various physical tests like diameter, thickness, uniformity of weight, hardness, friability, and drug content. The results of all these tests were found to be satisfactory. The in vitro dissolution study was carried out for 12 hours using paddle method in phosphate buffer (pH 6.8) as dissolution media. Formulation F1 to F3 failed to sustain release beyond 8 hours. Among all the formulation, F4 shows 99.15% of drug release at the end of 1...
A simple, precise economical and fast visible spectrophotometric method has been developed for th... more A simple, precise economical and fast visible spectrophotometric method has been developed for the determination of Itopride hydrochloride in tablet dosage form. Developed is based on formation of extractable colored complex of drug with coloring agent mordant blue 3. A wavelength maximum was found to 471.0 nm. Linearity was observed 30-70 mg /mL. The proposed method describes the determination of Itopride hydrochloride by visible spectrophotometric method which is a precise and selective. The result of analysis have been validated statistically and also by recovery studies.
Central nervous system agents in medicinal chemistry, 2021
BACKGROUND Benzothiazole is an organosulfur heterocyclic compound that has a considerable place i... more BACKGROUND Benzothiazole is an organosulfur heterocyclic compound that has a considerable place in drug discovery due to significant pharmacological actions. OBJECTIVE The main objective of the present study was to synthesize some novel 2-(5-substituted 1,3,4-oxadiazole-2-yl)-1,3-benzothiazole derivatives and evaluate them for their anticonvulsant activity using in silico and in vivo methods. METHOD A set of sixteen 2-(5-substituted 1, 3, 4-oxadiazole-2-yl)-1, 3-benzothiazole derivatives were prepared using multi-step reactions starting from o-amino-thiophenol and characterized by suitable spectral techniques. The synthesized compounds were evaluated for anticonvulsant activity using in silico and in vivo methods. In silico molecular docking study was performed using Molegro Virtual Docker software to analyze binding modes of compounds with the internal ligand of PDB ID: 1OHY and 1OHV; and in vivo pharmacological activities were tested for both generalized tonic-clonic seizures and ...
Immunomodulators are becoming very popular in the worldwide natural health industry as people sta... more Immunomodulators are becoming very popular in the worldwide natural health industry as people start to realize the importance of a healthy immune system in the maintenance of health and the prevention and recovery of disease. Help the immune system, and the body helps itself -often quite considerably. An immunomodulator, also known as an immunotherapy is a substance (e.g. a drug) which has an effect on the immune system. Immunotherapy is an approach that has been actively investigated in recent years as a method for disease prevention. It does not involve recognition of a specific antigen or targeting the immune response towards a specific pathogen, but causes an overall immune response that hastens recognition of foreign proteins. This review gives a brief introduction of various immunomodulators.
Summary The aim of this study was to formulate and evaluate the herbal face cream containing extr... more Summary The aim of this study was to formulate and evaluate the herbal face cream containing extracts of Cyperus rotundus, Cucumis sativus and almond oil. Different types of formulations oil in water (O/W) herbal creams namely F1 to F7 were formulated from the ethanol extract of Cyperus rotundus (roots) , Cucumis sativus (fruits) and almond oil in varied concentrations. All the seven formulations (F1 to F7) was evaluated for various parametrs like pH, viscosity, spreadability, rheological study, and stability along with irritancy test were examined. Formulations F4 and F5 showed good spreadability, good consistency, homogeneity, appearance, pH, ease of removal, spreadibilty and no evidence of phase separation. The formulation F4 and F5 shows no redness, edema, inflammation and irritation during irritancy studies. These formulations are safe to use for skin.
Ethanolic extract of the Mitragyna parvifolia was evaluated for antiinflammatory, analgesic and a... more Ethanolic extract of the Mitragyna parvifolia was evaluated for antiinflammatory, analgesic and antimicrobial activities. The extract showed very significant analgesic and anti-inflammatory potential. The analgesic activity was significant at the dose of 500 mg/kg (P< 0.01) while the doses of 250 and 100 mg/kg showed only promising results. The extract at the dose of 500 mg/Kg showed very high % inhibition in edema volume comparable to standard drug Diclofenac sodium (50 mg/Kg, i.p.). The plant extract did not exhibit any anti-bacterial potential against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa.
A series of 2-(4-aminophenyl)benzimidazole (2a) based acid / 2-hydrazinobenzimidazole (2b) with t... more A series of 2-(4-aminophenyl)benzimidazole (2a) based acid / 2-hydrazinobenzimidazole (2b) with the help of hydrazine hydrate which were then reacted with substituted sulfonyl chloride (4a-4f) and mixture of acetic anhydride, pyridine N-(4-(benzimidazole-2-yl)phenyl) sulfonamides, N'-(1H-benzimidazol-2-yl)phenyl hydrazido sulfonamides (5a-5l), respectively. The newly synthesized compounds were screened for their in-vitro biological activities including antimicrobial, and antioxidant activity. The Acetyl-CoA carboxylase (ACCase) inhibitor behavior of synthesized compounds was pre-assed via automated docking studies. Finally the whole effort leads to total 10 most promising analogues (5a, 5b, 5c, 5d, 5e, 5f, 5i, 5j, 5k, and 5l) which can be explored further as a template to design more potential agents against ACCase inhibitors.
International Journal of Pharmaceutical Sciences and Drug Research, 2020
Bombax ceiba plant belongs to bombacaceae family and is commonly known as Semal (Hindi) and Cotto... more Bombax ceiba plant belongs to bombacaceae family and is commonly known as Semal (Hindi) and Cotton tree (English). It has numerous effects like stimulant, astringent, haemostatic, diuretics, antidiarrhoeal, emeticand antipyretic. Major pharmacological activities reported in this plant are hypoglycemic, antianxiety, antibacterial, antiviral and anti-inflammatory. Numerous side effects and increased resistance to anthelmintic drugs prompted us to discover cost effective safe formulation of conventional medicinal plants. In the present study, research work is focused to evaluate the possible anthelmintic effects of Bombax ceiba. To investigate anthelmintic potential of Bombax ceiba plant, different extracts from dried powder stem bark were tested on adult Indian earthworms (Pheretima posthuma) having physiological & anatomical resemblance with human intestinal roundworm parasites. The drugs were divided in 14 groups consisting of test, standard and control. Each group was consisting of...
International Journal of Pharmaceutical Sciences and Drug Research, 2010
Matricaria recutita, once it has been called as Marticaria chamomilla, Chamomilla recutita, and C... more Matricaria recutita, once it has been called as Marticaria chamomilla, Chamomilla recutita, and Chamomilum nobile family Asteraceae. The main constituents of this plant include the terpenoids α-bisabolol and its oxides and azulenes, including chamazulene. Matricaria recutita shows different pharmacological activities like anti-inflammatory, anti- cancer, treatment of stress and depression, anti-allergic etc. This review focuses on the detailed chemical constituents, pharmacological activities of different parts of this plant.
Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellen... more Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellent tolerability. Orally it is rapidly absorbed and metabolized to sulfoxide and sulfone, which may be responsible for its anthelmenthic action. Single dose administration of albendazole has produced cure rates in ascarisis, hookworm and enterobiasis which are comparable to three day treatment with mebendazole. Albendazole chewable tablets (400 mg) were prepared by three methods viz. non aqueous granulation, aqueous granulation and direct compression and were named as NAG, AG and DC respectively. Tablet prepared by these three methods were evaluated by different parameters such as average weight, hardness, carr’s index, tapped density, friability, disintegration, content uniformity test, in vitro dissolution etc. All the parameters were found within the specifications. The study on the dissolution profile revealed that product ‘DC’ had faster dissolution rate while compared to remaining ba...
Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellen... more Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellent tolerability. Orally it is rapidly absorbed and metabolized to sulfoxide and sulfone, which may be responsible for its anthelmenthic action. Single dose administration of albendazole has produced cure rates in ascarisis, hookworm and enterobiasis which are comparable to three day treatment with mebendazole. Albendazole chewable tablets (400 mg) were prepared by three methods viz. non aqueous granulation, aqueous granulation and direct compression and were named as NAG, AG and DC respectively. Tablet prepared by these three methods were evaluated by different parameters such as average weight, hardness, carr’s index, tapped density, friability, disintegration, content uniformity test, in vitro dissolution etc. All the parameters were found within the specifications. The study on the dissolution profile revealed that product ‘DC’ had faster dissolution rate while compared to remaining ba...
We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a ... more We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a benzothiazole moiety. The title compounds in the two series namely N-(4-(benzothiazole-2-yl) phenyl) 4- substituted benzene sulfonamides and N-(4-(benzothiazole-2-yl) phenyl) 3- substituted benzene sulfonamides were synthesized by condensing 2-(3/4-aminophenyl) benzothiazole with various substituted sulfonyl chlorides. The synthesized compounds were subjected to neurotoxicity screening, computational studies, and evaluation of their anticonvulsant potential. Amongst all the synthesized compounds, compound 9 emerged as the most potent anticonvulsant agent in maximal electroshock (MES) model (standard: phenytoin) in mice and showed three hydrogen bond interactions with the nicotinic acetylcholine ion gated receptors (PDB ID: 2BG9). Interestingly, compound 13 showed five hydrogen bond interactions with the target protein and thus excellent binding affinity upon computational analysis but wa...
The aerial and root extracts of Artemisia dracunculus were subjected to screening of antidiabetic... more The aerial and root extracts of Artemisia dracunculus were subjected to screening of antidiabetic activity in Streptozotocin (STZ)-induced diabetic rats. The ethanol and aqueous extracts (250 mg/kg body weight) were administered orally in diabetic rats. After the oral administration of ethanol and aqueous extracts of aerial and root of Artemisia dracunculus, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. In the same study the action of the extracts on diabetes induced hyperlipidemia was analyzed where the extracts significantly lowered the elevated total cholesterol, triglycerides (TGL) and low density lipoprotein (LDL) level while increased the High density lipoprotein (HDL). Glibenclamide was used as a standard drug at a dose of 0.25 mg/kg. The experimental data revealed that extracts of aerial and root of Artemisia dracunculus has significant antihyperglycemic activity in Streptozotocin-induced rats compared to the s...
The objective of present work was to prepare and evaluate the long-term stability of W/O/W multip... more The objective of present work was to prepare and evaluate the long-term stability of W/O/W multiple emulsion with respect to the concentrations of Span 80 and Tween 80. In addition, the effect of surfactant, complexing agent, on rheological properties of emulsion was investigated. Scanning electron microscopy (SEM), zetasizer, zeta potential measurement, encapsulation efficiency and rheological properties is usually determined. It has been observed that phase separation values decreased, when increasing the concentration of Span 80, whereas Tween 80 concentration kept constant. On increasing Tween concentration, whereas Span 80 was kept constant, the phase separation was significantly increased. Hence it was selected to use high concentration of Span 80 i.e. 15% as lipophilic emulsifier, while low concentration of Tween 80 i.e. 0.1% as hydrophilic emulsifier for the further development of emulsion formulation. The stability of the formulation was assessed via microscopic observation...
Summary Sustained release formulation of Metformin HCl presents the formulator with significant c... more Summary Sustained release formulation of Metformin HCl presents the formulator with significant challenges due to its poor inherent compressibility, high dose and high water solubility. The objective of the present study was to develop sustained release matrix tablets of Metformin HCl, an anti diabetic drug. The sustained release tablets were prepared by direct compression method and formulated using different drug and polymer ratios, formulations such as F1 to F6. Polymers like Sodium carboxymethyl cellulos (Sod. CMC), hydroxyl propyl methyl cellulose (HPMCK�100), Xanthan gum and HPMCK�4 were used. Tablets blends were evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. The compressed tablets were then evaluated for various physical tests like diameter, thickness, uniformity of weight, hardness, friability, and drug content. The results of all these tests were found to be satisfactory. The in vitro dissolution...
Background A large number of studies have recently reported that, because of their significant bi... more Background A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue. Main text This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc.. Conclusion This review highlights the current status of triazole compounds as different multi-target ph...
Context: Virtual screening techniques or computational methods are used for the drug discovery an... more Context: Virtual screening techniques or computational methods are used for the drug discovery and development. Objective: In search for the safer and effective anticonvulsant agents, docking study on pyridazinone derivatives was performed to potentiate GABA mediated chlorine channel opening. Methods: A total of eighteen compounds were screened for their anticonvulsant activity using molecular docking inside the ligand binding domain of PDB ID 2Q1Q using Molegro Virtual docker. QikProp 3.4 & molinspiration software were also used to evaluate drug likeliness and to perform comparative bioactivity analysis for all the pyridazinone derivatives. Results: Out of eighteen compounds, (I) showed highest Mol dock score and (XVIII) formed maximum number of hydrogen bond interactions. Oxygen atom of the Nitro group on the biphenyl ring of compound (XV) formed a strong hydrogen bond with Thr199 with a distance 2.33?. Mol dock score of diazepam (standard drug) was -101.5306. Conclusions: Based on the results of mol dock score and number of hydrogen bond interactions, compounds (XVIII) and (XIII) observed to be the most potent compounds.
Benzothiazole is one of the promising heterocyclic compounds in the medicinal chemistry, endowed ... more Benzothiazole is one of the promising heterocyclic compounds in the medicinal chemistry, endowed with several therapeutic potentials. The present research endeavors the high throughput in silico screening of 66 designed benzothiazole derivatives as potent GABA-aminotransferase inhibitors in Molegro virtual docker software (Version 6.0) using 1OHV as PDB. The docking results showed mol dock score of-73.63 and-62.45 for the standard drugs phenytoin and carbamazepine respectively, on the other hand, the benzothiazole derivatives SDZ3,
1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as t... more 1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as they have wide variety of biological activities. 1, 3, 4-oxadiazole derivatives exhibited noteworthy anticancer activities. In recent years, microwave-induced organic reactions attained significant attention due to several benefits, such as short reaction time, cost-effectiveness, excellent yield, and ease of work. In view of above in present work, SAR and mechanism of action of 1, 3, 4-oxadiazole derivatives as anticancer agents, reported by different research groups in recent years are summarized. Present review also highlighted the various synthetic approaches for efficient microwave-assisted green synthesis of 1, 3, 4-oxadiazole derivatives.
Central Nervous System Agents in Medicinal Chemistry, 2022
Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics med... more Background: Malaria parasite strains are resistant to the therapeutic effect of prophylactics medicines presently available. This resistance now poses a significant challenge to researchers to beat malaria parasitic infections. Strategies such as investigating newer hybrid chemical entities and specified drug targets may help us spot new efficient derivatives that bind to the parasites in a more specific manner and inhibit their growth. Objective: To scientifically perform the experimental, pharmacological, and computational studies of pyrazole-based furanone hybrids as novel antimalarial agents. Methods: A series of new furanone-based pyrazole derivatives were synthesized and investigated as potential antimalarial agents by performing in vitro antimalarial activity. To get further optimization, these synthesized derivatives were virtually screened based on ADME-T filters, and molecular docking studies were also accomplished on the crystal structures of Plasmodium falciparum lactate...
Summary The objective of this study was to formulate and evaluate Salbutamol sulphate matrix tabl... more Summary The objective of this study was to formulate and evaluate Salbutamol sulphate matrix tablets, sustained release dosage form, for the treatment of Chronic Obstructive Pulmonary Disease (COPD). The matrix tablets were prepared by direct comression method using two polymers such as hydroxyl propyl methyl cellulose (HPMC) and xanthan gum in varying ratios. Tablets blends were evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. The compressed tablets were then evaluated for various physical tests like diameter, thickness, uniformity of weight, hardness, friability, and drug content. The results of all these tests were found to be satisfactory. The in vitro dissolution study was carried out for 12 hours using paddle method in phosphate buffer (pH 6.8) as dissolution media. Formulation F1 to F3 failed to sustain release beyond 8 hours. Among all the formulation, F4 shows 99.15% of drug release at the end of 1...
A simple, precise economical and fast visible spectrophotometric method has been developed for th... more A simple, precise economical and fast visible spectrophotometric method has been developed for the determination of Itopride hydrochloride in tablet dosage form. Developed is based on formation of extractable colored complex of drug with coloring agent mordant blue 3. A wavelength maximum was found to 471.0 nm. Linearity was observed 30-70 mg /mL. The proposed method describes the determination of Itopride hydrochloride by visible spectrophotometric method which is a precise and selective. The result of analysis have been validated statistically and also by recovery studies.
Central nervous system agents in medicinal chemistry, 2021
BACKGROUND Benzothiazole is an organosulfur heterocyclic compound that has a considerable place i... more BACKGROUND Benzothiazole is an organosulfur heterocyclic compound that has a considerable place in drug discovery due to significant pharmacological actions. OBJECTIVE The main objective of the present study was to synthesize some novel 2-(5-substituted 1,3,4-oxadiazole-2-yl)-1,3-benzothiazole derivatives and evaluate them for their anticonvulsant activity using in silico and in vivo methods. METHOD A set of sixteen 2-(5-substituted 1, 3, 4-oxadiazole-2-yl)-1, 3-benzothiazole derivatives were prepared using multi-step reactions starting from o-amino-thiophenol and characterized by suitable spectral techniques. The synthesized compounds were evaluated for anticonvulsant activity using in silico and in vivo methods. In silico molecular docking study was performed using Molegro Virtual Docker software to analyze binding modes of compounds with the internal ligand of PDB ID: 1OHY and 1OHV; and in vivo pharmacological activities were tested for both generalized tonic-clonic seizures and ...
Immunomodulators are becoming very popular in the worldwide natural health industry as people sta... more Immunomodulators are becoming very popular in the worldwide natural health industry as people start to realize the importance of a healthy immune system in the maintenance of health and the prevention and recovery of disease. Help the immune system, and the body helps itself -often quite considerably. An immunomodulator, also known as an immunotherapy is a substance (e.g. a drug) which has an effect on the immune system. Immunotherapy is an approach that has been actively investigated in recent years as a method for disease prevention. It does not involve recognition of a specific antigen or targeting the immune response towards a specific pathogen, but causes an overall immune response that hastens recognition of foreign proteins. This review gives a brief introduction of various immunomodulators.
Summary The aim of this study was to formulate and evaluate the herbal face cream containing extr... more Summary The aim of this study was to formulate and evaluate the herbal face cream containing extracts of Cyperus rotundus, Cucumis sativus and almond oil. Different types of formulations oil in water (O/W) herbal creams namely F1 to F7 were formulated from the ethanol extract of Cyperus rotundus (roots) , Cucumis sativus (fruits) and almond oil in varied concentrations. All the seven formulations (F1 to F7) was evaluated for various parametrs like pH, viscosity, spreadability, rheological study, and stability along with irritancy test were examined. Formulations F4 and F5 showed good spreadability, good consistency, homogeneity, appearance, pH, ease of removal, spreadibilty and no evidence of phase separation. The formulation F4 and F5 shows no redness, edema, inflammation and irritation during irritancy studies. These formulations are safe to use for skin.
Ethanolic extract of the Mitragyna parvifolia was evaluated for antiinflammatory, analgesic and a... more Ethanolic extract of the Mitragyna parvifolia was evaluated for antiinflammatory, analgesic and antimicrobial activities. The extract showed very significant analgesic and anti-inflammatory potential. The analgesic activity was significant at the dose of 500 mg/kg (P< 0.01) while the doses of 250 and 100 mg/kg showed only promising results. The extract at the dose of 500 mg/Kg showed very high % inhibition in edema volume comparable to standard drug Diclofenac sodium (50 mg/Kg, i.p.). The plant extract did not exhibit any anti-bacterial potential against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa.
A series of 2-(4-aminophenyl)benzimidazole (2a) based acid / 2-hydrazinobenzimidazole (2b) with t... more A series of 2-(4-aminophenyl)benzimidazole (2a) based acid / 2-hydrazinobenzimidazole (2b) with the help of hydrazine hydrate which were then reacted with substituted sulfonyl chloride (4a-4f) and mixture of acetic anhydride, pyridine N-(4-(benzimidazole-2-yl)phenyl) sulfonamides, N'-(1H-benzimidazol-2-yl)phenyl hydrazido sulfonamides (5a-5l), respectively. The newly synthesized compounds were screened for their in-vitro biological activities including antimicrobial, and antioxidant activity. The Acetyl-CoA carboxylase (ACCase) inhibitor behavior of synthesized compounds was pre-assed via automated docking studies. Finally the whole effort leads to total 10 most promising analogues (5a, 5b, 5c, 5d, 5e, 5f, 5i, 5j, 5k, and 5l) which can be explored further as a template to design more potential agents against ACCase inhibitors.
International Journal of Pharmaceutical Sciences and Drug Research, 2020
Bombax ceiba plant belongs to bombacaceae family and is commonly known as Semal (Hindi) and Cotto... more Bombax ceiba plant belongs to bombacaceae family and is commonly known as Semal (Hindi) and Cotton tree (English). It has numerous effects like stimulant, astringent, haemostatic, diuretics, antidiarrhoeal, emeticand antipyretic. Major pharmacological activities reported in this plant are hypoglycemic, antianxiety, antibacterial, antiviral and anti-inflammatory. Numerous side effects and increased resistance to anthelmintic drugs prompted us to discover cost effective safe formulation of conventional medicinal plants. In the present study, research work is focused to evaluate the possible anthelmintic effects of Bombax ceiba. To investigate anthelmintic potential of Bombax ceiba plant, different extracts from dried powder stem bark were tested on adult Indian earthworms (Pheretima posthuma) having physiological & anatomical resemblance with human intestinal roundworm parasites. The drugs were divided in 14 groups consisting of test, standard and control. Each group was consisting of...
International Journal of Pharmaceutical Sciences and Drug Research, 2010
Matricaria recutita, once it has been called as Marticaria chamomilla, Chamomilla recutita, and C... more Matricaria recutita, once it has been called as Marticaria chamomilla, Chamomilla recutita, and Chamomilum nobile family Asteraceae. The main constituents of this plant include the terpenoids α-bisabolol and its oxides and azulenes, including chamazulene. Matricaria recutita shows different pharmacological activities like anti-inflammatory, anti- cancer, treatment of stress and depression, anti-allergic etc. This review focuses on the detailed chemical constituents, pharmacological activities of different parts of this plant.
Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellen... more Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellent tolerability. Orally it is rapidly absorbed and metabolized to sulfoxide and sulfone, which may be responsible for its anthelmenthic action. Single dose administration of albendazole has produced cure rates in ascarisis, hookworm and enterobiasis which are comparable to three day treatment with mebendazole. Albendazole chewable tablets (400 mg) were prepared by three methods viz. non aqueous granulation, aqueous granulation and direct compression and were named as NAG, AG and DC respectively. Tablet prepared by these three methods were evaluated by different parameters such as average weight, hardness, carr’s index, tapped density, friability, disintegration, content uniformity test, in vitro dissolution etc. All the parameters were found within the specifications. The study on the dissolution profile revealed that product ‘DC’ had faster dissolution rate while compared to remaining ba...
Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellen... more Albendazole is a benzimidazole derivative with broad spectrum anthelmenthic activity and excellent tolerability. Orally it is rapidly absorbed and metabolized to sulfoxide and sulfone, which may be responsible for its anthelmenthic action. Single dose administration of albendazole has produced cure rates in ascarisis, hookworm and enterobiasis which are comparable to three day treatment with mebendazole. Albendazole chewable tablets (400 mg) were prepared by three methods viz. non aqueous granulation, aqueous granulation and direct compression and were named as NAG, AG and DC respectively. Tablet prepared by these three methods were evaluated by different parameters such as average weight, hardness, carr’s index, tapped density, friability, disintegration, content uniformity test, in vitro dissolution etc. All the parameters were found within the specifications. The study on the dissolution profile revealed that product ‘DC’ had faster dissolution rate while compared to remaining ba...
We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a ... more We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a benzothiazole moiety. The title compounds in the two series namely N-(4-(benzothiazole-2-yl) phenyl) 4- substituted benzene sulfonamides and N-(4-(benzothiazole-2-yl) phenyl) 3- substituted benzene sulfonamides were synthesized by condensing 2-(3/4-aminophenyl) benzothiazole with various substituted sulfonyl chlorides. The synthesized compounds were subjected to neurotoxicity screening, computational studies, and evaluation of their anticonvulsant potential. Amongst all the synthesized compounds, compound 9 emerged as the most potent anticonvulsant agent in maximal electroshock (MES) model (standard: phenytoin) in mice and showed three hydrogen bond interactions with the nicotinic acetylcholine ion gated receptors (PDB ID: 2BG9). Interestingly, compound 13 showed five hydrogen bond interactions with the target protein and thus excellent binding affinity upon computational analysis but wa...
The aerial and root extracts of Artemisia dracunculus were subjected to screening of antidiabetic... more The aerial and root extracts of Artemisia dracunculus were subjected to screening of antidiabetic activity in Streptozotocin (STZ)-induced diabetic rats. The ethanol and aqueous extracts (250 mg/kg body weight) were administered orally in diabetic rats. After the oral administration of ethanol and aqueous extracts of aerial and root of Artemisia dracunculus, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. In the same study the action of the extracts on diabetes induced hyperlipidemia was analyzed where the extracts significantly lowered the elevated total cholesterol, triglycerides (TGL) and low density lipoprotein (LDL) level while increased the High density lipoprotein (HDL). Glibenclamide was used as a standard drug at a dose of 0.25 mg/kg. The experimental data revealed that extracts of aerial and root of Artemisia dracunculus has significant antihyperglycemic activity in Streptozotocin-induced rats compared to the s...
The objective of present work was to prepare and evaluate the long-term stability of W/O/W multip... more The objective of present work was to prepare and evaluate the long-term stability of W/O/W multiple emulsion with respect to the concentrations of Span 80 and Tween 80. In addition, the effect of surfactant, complexing agent, on rheological properties of emulsion was investigated. Scanning electron microscopy (SEM), zetasizer, zeta potential measurement, encapsulation efficiency and rheological properties is usually determined. It has been observed that phase separation values decreased, when increasing the concentration of Span 80, whereas Tween 80 concentration kept constant. On increasing Tween concentration, whereas Span 80 was kept constant, the phase separation was significantly increased. Hence it was selected to use high concentration of Span 80 i.e. 15% as lipophilic emulsifier, while low concentration of Tween 80 i.e. 0.1% as hydrophilic emulsifier for the further development of emulsion formulation. The stability of the formulation was assessed via microscopic observation...
Summary Sustained release formulation of Metformin HCl presents the formulator with significant c... more Summary Sustained release formulation of Metformin HCl presents the formulator with significant challenges due to its poor inherent compressibility, high dose and high water solubility. The objective of the present study was to develop sustained release matrix tablets of Metformin HCl, an anti diabetic drug. The sustained release tablets were prepared by direct compression method and formulated using different drug and polymer ratios, formulations such as F1 to F6. Polymers like Sodium carboxymethyl cellulos (Sod. CMC), hydroxyl propyl methyl cellulose (HPMCK�100), Xanthan gum and HPMCK�4 were used. Tablets blends were evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. The compressed tablets were then evaluated for various physical tests like diameter, thickness, uniformity of weight, hardness, friability, and drug content. The results of all these tests were found to be satisfactory. The in vitro dissolution...
Background A large number of studies have recently reported that, because of their significant bi... more Background A large number of studies have recently reported that, because of their significant biological and pharmacological properties, heterocyclic compounds and their derivatives have attracted a strong interest in medicinal chemistry. The triazole nucleus is one of the most important heterocycles which has a feature of natural products as well as medicinal agents. Heterocyclic nitrogen is abundantly present in most medicinal compounds. The derivatization of triazole ring is based on the phenomenon of bio-isosteres in which substituted the oxygen atom of oxadiazole nucleus with nitrogen triazole analogue. Main text This review focuses on recent synthetic procedure of triazole moiety, which comprises of various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc.. Conclusion This review highlights the current status of triazole compounds as different multi-target ph...
Context: Virtual screening techniques or computational methods are used for the drug discovery an... more Context: Virtual screening techniques or computational methods are used for the drug discovery and development. Objective: In search for the safer and effective anticonvulsant agents, docking study on pyridazinone derivatives was performed to potentiate GABA mediated chlorine channel opening. Methods: A total of eighteen compounds were screened for their anticonvulsant activity using molecular docking inside the ligand binding domain of PDB ID 2Q1Q using Molegro Virtual docker. QikProp 3.4 & molinspiration software were also used to evaluate drug likeliness and to perform comparative bioactivity analysis for all the pyridazinone derivatives. Results: Out of eighteen compounds, (I) showed highest Mol dock score and (XVIII) formed maximum number of hydrogen bond interactions. Oxygen atom of the Nitro group on the biphenyl ring of compound (XV) formed a strong hydrogen bond with Thr199 with a distance 2.33?. Mol dock score of diazepam (standard drug) was -101.5306. Conclusions: Based on the results of mol dock score and number of hydrogen bond interactions, compounds (XVIII) and (XIII) observed to be the most potent compounds.
Benzothiazole is one of the promising heterocyclic compounds in the medicinal chemistry, endowed ... more Benzothiazole is one of the promising heterocyclic compounds in the medicinal chemistry, endowed with several therapeutic potentials. The present research endeavors the high throughput in silico screening of 66 designed benzothiazole derivatives as potent GABA-aminotransferase inhibitors in Molegro virtual docker software (Version 6.0) using 1OHV as PDB. The docking results showed mol dock score of-73.63 and-62.45 for the standard drugs phenytoin and carbamazepine respectively, on the other hand, the benzothiazole derivatives SDZ3,
1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as t... more 1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as they have wide variety of biological activities. 1, 3, 4-oxadiazole derivatives exhibited noteworthy anticancer activities. In recent years, microwave-induced organic reactions attained significant attention due to several benefits, such as short reaction time, cost-effectiveness, excellent yield, and ease of work. In view of above in present work, SAR and mechanism of action of 1, 3, 4-oxadiazole derivatives as anticancer agents, reported by different research groups in recent years are summarized. Present review also highlighted the various synthetic approaches for efficient microwave-assisted green synthesis of 1, 3, 4-oxadiazole derivatives.
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Papers by sukhbir khokra