Novel oxino bis-pyrazoles were obtained by two step reactions of 3-methyl-1-phenyl pyrazoline-5-o... more Novel oxino bis-pyrazoles were obtained by two step reactions of 3-methyl-1-phenyl pyrazoline-5-one, cyanoacetamide and aryl-or alkylaldehydes, in the presence of catalytic amounts of triethylamine and ethanol as a solvent. All the synthesized compounds were evaluated for their inhibitory activities against butyrylcholinesterase (BChE) and bovine α-chymotrypsin. Two compounds, 8 and 9 were found to be good inhibitors of enzyme BChE with IC50 values of 52.74 ± 0.006 and 51.85 ± 0.005 µM, respectively.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and thei... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their α-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC50 = 37.38±0.12μM), all synthesized compounds showed potent activity with IC50 values between 31.26±0.11 to 396.25±0.18μM. The most potent compounds 6, 8 and 11 showed IC50 values within the range of 31.26±0.11 to 37.48±0.12μM. Compounds 7, 10, 12 and 13 showed IC50 values within the range of 65.23±0.12 to 154.87±0.16μM, while compounds 4, 5 and 9 showed moderate inhibition with IC50 values 286.56±0.16 to 396.25±0.18μM. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a crucial role in...
Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vi... more Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vitro cholinesterases (AChE, BChE) inhibitory activity. All compounds showed potent activity with IC50 values between 0.21±0.003 to 147.14±0.12μM for AChE and among them five compounds showed potent activity with IC50 values 17.16±0.02 to 231.6±0.12μM for BChE when compared with standard Eserine (IC50 = 0.85±0.0001 μM (AChE) & 0.04±0.0001μM (BChE). The most potent compound 11 can be considered as potential lead compound showed an inhibition of 95.35±0.11 and IC50= 0.21±0.003 while compound 7 showed an inhibition of 83.45±0.13 and IC50= 17.16±0.02. It is concluded from structural activity relationship that the presence of nitro group at C-2 and C-4 position of dihydropyridine ring increase the acetyl cholinesterase and butyrylcholinesterase activities of these compounds while presence of -Br and -Cl also enhances the activities.
Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocycl... more Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocyclic compounds carries a unique place in chemical synthesis. Biginelli reaction, among the loop of multicomponent reactions, provide an efficient way to access of highly functionalized dihydropyrimidones (-thiones) (DHPMs). In the current study, we employed multicomponent Biginelli reaction to synthesis range of different dihydropyrimidones (-thiones) derivatives in variable yields. A solvent-free eco-friendly green protocol without any expensive catalyst has been optimized and expand to synthesize series of DHMPS in 34 to 72% yield. The optimized method proved to be successful with various types of different aromatic aldehydes, 1, 3-dicarbonyl compounds and urea (thiourea) under solvent and catalyst free condition to access dihydropyrimidones (-thiones). Different spectroscopic techniques include NMR, FTIR etc. have used to confirm the structures of compounds. Further exploration of Biginelli reaction to prepare DHPMs and related compounds is under way in the lab and will be published in due course.
The transition metal complexes of Co(II), Ni(II), and Cu(II) derived from N'-((5-(2,5-dichlor... more The transition metal complexes of Co(II), Ni(II), and Cu(II) derived from N'-((5-(2,5-dichlorophenyl)furan-2-yl)methylene)-2-hydroxybenzohydrazide (L24) and N'-((5-(2, 5-dichlorophenyl)furan-2-yl)methylene)benzohydrazide (L21) have been synthesized by conventional as well as microwave method being shorter time consuming, solvent less and gives improved yields as compared to the traditional conventional technique. These compounds were characterized by melting point, TLC, FTIR, 1H-NMR, elemental analysis, potentiometric titration, ICP-OES and EIMS. From this analytical data it is confirmed that complexes are in octahedral structure with coordination number 6 which revealed 1:2 (metal:ligand). FTIR data shows that these synthesized hydrazone ligands have ONO donor sites and coordinate with transition metal ions in a tridentate monobasic manner. All these synthesized compounds were tested for evaluation of antibacterial activity by agar disc diffusion assay and total antioxidant...
Detection of individual metal ions is of importance across a range of fields of chemistry includi... more Detection of individual metal ions is of importance across a range of fields of chemistry including environmental monitoring, and health and disease. Fluorescence is a highly sensitive technique and small fluorescent molecules are widely used for the detection and quantification of metal ions in various applications. Achieving specificity for a single metal from a single sensor is always a challenge. An alternative to selective sensing is the use of a number of non-specific sensors, in an array, which together respond in a unique pattern to each analyte. Here we show that screening a library of compounds can give a small sensor set that can be used to identify a range of metal ions following PCA and LDA. We explore a method for screening the initial compounds to identify the best performing sensors. We then present our method for reducing the size of the sensor array, resulting in a four-membered system, which is capable of identifying nine distinct metal ion species in lake water.
Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocycl... more Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocyclic compounds carries a unique place in chemical synthesis. Biginelli reaction, among the loop of multicomponent reactions, provide an efficient way to access of highly functionalized dihydropyrimidones (-thiones) (DHPMs). In the current study, we employed multicomponent Biginelli reaction to synthesis range of different dihydropyrimidones (-thiones) derivatives in variable yields. A solvent-free eco-friendly green protocol without any expensive catalyst has been optimized and expand to synthesize series of DHMPS in 34 to 72% yield. The optimized method proved to be successful with various types of different aromatic aldehydes, 1, 3-dicarbonyl compounds and urea (thiourea) under solvent and catalyst free condition to access dihydropyrimidones (-thiones). Different spectroscopic techniques include NMR, FTIR etc. have used to confirm the structures of compounds. Further exploration of Biginelli reaction to prepare DHPMs and related compounds is under way in the lab and will be published in due course.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase ... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1 H-NMR, 13 C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC 50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC 50 values between 31.26±0.11 to 396.25±0.18 M. The most potent compounds 6, 8 and 11 showed IC 50 values within the range of 31.26±0.11 to 37.48±0.12 M. Compounds 7, 10, 12 and 13 showed IC 50 values within the range of 65.23±0.12 to 154.87±0.16 M, while compounds 4, 5 and 9 showed moderate inhibition with IC 50 values 286.56±0.16 to 396.25±0.18 M. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a -glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest antihemolytic activity while 8 showed low anti-hemolytic and high hemolytic activity.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase ... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1 H-NMR, 13 C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC 50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC 50 values between 31.26±0.11 to 396.25±0.18 M. The most potent compounds 6, 8 and 11 showed IC 50 values within the range of 31.26±0.11 to 37.48±0.12 M. Compounds 7, 10, 12 and 13 showed IC 50 values within the range of 65.23±0.12 to 154.87±0.16 M, while compounds 4, 5 and 9 showed moderate inhibition with IC 50 values 286.56±0.16 to 396.25±0.18 M. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a -glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest antihemolytic activity while 8 showed low anti-hemolytic and high hemolytic activity.
Novel oxino bis-pyrazoles were obtained by two step reactions of 3-methyl-1-phenyl pyrazoline-5-o... more Novel oxino bis-pyrazoles were obtained by two step reactions of 3-methyl-1-phenyl pyrazoline-5-one, cyanoacetamide and aryl-or alkylaldehydes, in the presence of catalytic amounts of triethylamine and ethanol as a solvent. All the synthesized compounds were evaluated for their inhibitory activities against butyrylcholinesterase (BChE) and bovine α-chymotrypsin. Two compounds, 8 and 9 were found to be good inhibitors of enzyme BChE with IC50 values of 52.74 ± 0.006 and 51.85 ± 0.005 µM, respectively.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and thei... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their α-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC50 = 37.38±0.12μM), all synthesized compounds showed potent activity with IC50 values between 31.26±0.11 to 396.25±0.18μM. The most potent compounds 6, 8 and 11 showed IC50 values within the range of 31.26±0.11 to 37.48±0.12μM. Compounds 7, 10, 12 and 13 showed IC50 values within the range of 65.23±0.12 to 154.87±0.16μM, while compounds 4, 5 and 9 showed moderate inhibition with IC50 values 286.56±0.16 to 396.25±0.18μM. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a crucial role in...
Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vi... more Twelve derivatives of dihydropyridine derivatives (6-17) were synthesized and evaluated for in-vitro cholinesterases (AChE, BChE) inhibitory activity. All compounds showed potent activity with IC50 values between 0.21±0.003 to 147.14±0.12μM for AChE and among them five compounds showed potent activity with IC50 values 17.16±0.02 to 231.6±0.12μM for BChE when compared with standard Eserine (IC50 = 0.85±0.0001 μM (AChE) & 0.04±0.0001μM (BChE). The most potent compound 11 can be considered as potential lead compound showed an inhibition of 95.35±0.11 and IC50= 0.21±0.003 while compound 7 showed an inhibition of 83.45±0.13 and IC50= 17.16±0.02. It is concluded from structural activity relationship that the presence of nitro group at C-2 and C-4 position of dihydropyridine ring increase the acetyl cholinesterase and butyrylcholinesterase activities of these compounds while presence of -Br and -Cl also enhances the activities.
Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocycl... more Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocyclic compounds carries a unique place in chemical synthesis. Biginelli reaction, among the loop of multicomponent reactions, provide an efficient way to access of highly functionalized dihydropyrimidones (-thiones) (DHPMs). In the current study, we employed multicomponent Biginelli reaction to synthesis range of different dihydropyrimidones (-thiones) derivatives in variable yields. A solvent-free eco-friendly green protocol without any expensive catalyst has been optimized and expand to synthesize series of DHMPS in 34 to 72% yield. The optimized method proved to be successful with various types of different aromatic aldehydes, 1, 3-dicarbonyl compounds and urea (thiourea) under solvent and catalyst free condition to access dihydropyrimidones (-thiones). Different spectroscopic techniques include NMR, FTIR etc. have used to confirm the structures of compounds. Further exploration of Biginelli reaction to prepare DHPMs and related compounds is under way in the lab and will be published in due course.
The transition metal complexes of Co(II), Ni(II), and Cu(II) derived from N'-((5-(2,5-dichlor... more The transition metal complexes of Co(II), Ni(II), and Cu(II) derived from N'-((5-(2,5-dichlorophenyl)furan-2-yl)methylene)-2-hydroxybenzohydrazide (L24) and N'-((5-(2, 5-dichlorophenyl)furan-2-yl)methylene)benzohydrazide (L21) have been synthesized by conventional as well as microwave method being shorter time consuming, solvent less and gives improved yields as compared to the traditional conventional technique. These compounds were characterized by melting point, TLC, FTIR, 1H-NMR, elemental analysis, potentiometric titration, ICP-OES and EIMS. From this analytical data it is confirmed that complexes are in octahedral structure with coordination number 6 which revealed 1:2 (metal:ligand). FTIR data shows that these synthesized hydrazone ligands have ONO donor sites and coordinate with transition metal ions in a tridentate monobasic manner. All these synthesized compounds were tested for evaluation of antibacterial activity by agar disc diffusion assay and total antioxidant...
Detection of individual metal ions is of importance across a range of fields of chemistry includi... more Detection of individual metal ions is of importance across a range of fields of chemistry including environmental monitoring, and health and disease. Fluorescence is a highly sensitive technique and small fluorescent molecules are widely used for the detection and quantification of metal ions in various applications. Achieving specificity for a single metal from a single sensor is always a challenge. An alternative to selective sensing is the use of a number of non-specific sensors, in an array, which together respond in a unique pattern to each analyte. Here we show that screening a library of compounds can give a small sensor set that can be used to identify a range of metal ions following PCA and LDA. We explore a method for screening the initial compounds to identify the best performing sensors. We then present our method for reducing the size of the sensor array, resulting in a four-membered system, which is capable of identifying nine distinct metal ion species in lake water.
Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocycl... more Applications of multicomponent reactions (MCRs) in the preparation of diverse types of heterocyclic compounds carries a unique place in chemical synthesis. Biginelli reaction, among the loop of multicomponent reactions, provide an efficient way to access of highly functionalized dihydropyrimidones (-thiones) (DHPMs). In the current study, we employed multicomponent Biginelli reaction to synthesis range of different dihydropyrimidones (-thiones) derivatives in variable yields. A solvent-free eco-friendly green protocol without any expensive catalyst has been optimized and expand to synthesize series of DHMPS in 34 to 72% yield. The optimized method proved to be successful with various types of different aromatic aldehydes, 1, 3-dicarbonyl compounds and urea (thiourea) under solvent and catalyst free condition to access dihydropyrimidones (-thiones). Different spectroscopic techniques include NMR, FTIR etc. have used to confirm the structures of compounds. Further exploration of Biginelli reaction to prepare DHPMs and related compounds is under way in the lab and will be published in due course.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase ... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1 H-NMR, 13 C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC 50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC 50 values between 31.26±0.11 to 396.25±0.18 M. The most potent compounds 6, 8 and 11 showed IC 50 values within the range of 31.26±0.11 to 37.48±0.12 M. Compounds 7, 10, 12 and 13 showed IC 50 values within the range of 65.23±0.12 to 154.87±0.16 M, while compounds 4, 5 and 9 showed moderate inhibition with IC 50 values 286.56±0.16 to 396.25±0.18 M. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a -glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest antihemolytic activity while 8 showed low anti-hemolytic and high hemolytic activity.
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase ... more In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1 H-NMR, 13 C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC 50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC 50 values between 31.26±0.11 to 396.25±0.18 M. The most potent compounds 6, 8 and 11 showed IC 50 values within the range of 31.26±0.11 to 37.48±0.12 M. Compounds 7, 10, 12 and 13 showed IC 50 values within the range of 65.23±0.12 to 154.87±0.16 M, while compounds 4, 5 and 9 showed moderate inhibition with IC 50 values 286.56±0.16 to 396.25±0.18 M. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a -glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest antihemolytic activity while 8 showed low anti-hemolytic and high hemolytic activity.
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