A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzene... more A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzenesulfonamide was designed following the tail approach as possible hCAIX inhibitors.
Abstract In an attempt to develop active antimicrobial agents, a set of new thiazolyl chalcones h... more Abstract In an attempt to develop active antimicrobial agents, a set of new thiazolyl chalcones has been synthesized by the Claisen–Schmidt reaction of 5-acetyl-4-methyl-2-(3-pyridyl)thiazole with various heterocyclic aldehydes in alkali media. Reaction of chalcones with hydrazine hydrate has resulted in pyrazolines that have been assessed for in vitro antimicrobial activity against ten bacterial and five fungal human pathogenic strains using the disk diffusion assay. The synthesized pyrazolines demonstrate antimicrobial activity higher than that of synthesized chalcones. 2-Thienylchalcone has been determined as the most active against P. aeruginosa . Three pyrazolines are characterized by distinctive activity towards Gram-negative bacteria S. flexneri and P. aeruginosa . Two pyrazolines demonstrate equipotent antifungal activity with amphotricin B against A. clavatus .
Toward finding potential and novel anticancer agents, we designed and prepared novel differently ... more Toward finding potential and novel anticancer agents, we designed and prepared novel differently substituted unsymmetrical azine-modified thiadiazole sulfonamide derivatives using the “combi-targeting approach”.
Lignosulfonate (LS) is a byproduct obtained from the sulfite pulping process, LS improves the phy... more Lignosulfonate (LS) is a byproduct obtained from the sulfite pulping process, LS improves the physical properties of several biopolymer as gelatin. On the other hand, the physicochemical modification of cellulose is a must for making it more applicable in several fields rather than paper or textile industries. Here, we report the fabrication of films derived from calcium lignosulfonate (Ca LS)/sodium cellulose composite for the first time. Which can be used in food packaging to preserve the quality and safety of the food. In order to characterize sodium cellulose and the synthesized composite films, Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM), and thermogravimetric analysis along with water vapor transmission and permeability tests were carried out. The XPS spectrum of sodium cellulose showed a sharp Na (1s) peak (1045 eV), which emphasized the presence of Na + ions. The FT-IR sp...
International Journal of Biological Macromolecules, 2019
N-allylthiourea chitosan (ATUCS), a chelating material, was prepared, characterized, and studied ... more N-allylthiourea chitosan (ATUCS), a chelating material, was prepared, characterized, and studied for the removal of arsenazo III ((As(III)) dye from aqueous solution. Scanning electron microscopy (SEM), energy-dispersive X-ray (EDX), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), and 1 Hand 13 Cnuclear magnetic resonance (NMR) were used to characterize the prepared adsorbent and to investigate the adsorption mechanism. Furthermore, the adsorption behavior of chitosan (CS) and ATUCS were studied under various conditions. The equilibrium adsorbed amount of As(III) onto ATUCS was found to be 116.3 mg/g, compared to 87.3 mg/g with respect to CS. The regeneration of the loaded CS and ATUCS were studied using 1:1 solution of H2O2-H2SO4 and reused with certain change in efficiency after the third cycle. The adsorption process was found to fit well with pseudo-second-order kinetic model. The equilibrium data were better described with the Freundlich isotherm. The monolayer adsorption capacity was found to be 204.08 and 90.90 mg/g for the As (III)/ATUCS and As (III)/CS systems, respectively, at 25 C. The pH of the higher uptake of As (III) onto ATUCS and CS was 4-5 and 8.0, respectively. The results demonstrated improved adsorption of As (III) using ATUCS as compared to the CS.
International Journal of Emerging Trends in Engineering and Development, 2018
The efficiency of two thiosemicarbazide derivatives; 4-phenyl-thiosemicarbazide and 4allyl-thiose... more The efficiency of two thiosemicarbazide derivatives; 4-phenyl-thiosemicarbazide and 4allyl-thiosemicarbazide as corrosion inhibitors against C-steel and its adsorption behavior were investigated in 2 M HCl solution using potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and electrochemical frequency modulation (EFM) techniques. Results revealed that the inhibition efficiency increased with the inhibitor concentration and also indicate both thiosemicarbazide derivatives act as mixed-type inhibitors. EIS spectra exhibit one capacitive loop and confirm the inhibitive ability. Quantum chemical calculations have been employed for the inhibition efficiency of these thiosemicarbazide derivatives for Csteel in aggressive acidic media by means of density functional theory (DFT) methods B3LYP/6-31g* in gas phase. The calculated quantum chemical parameters correlated to the inhibition efficiency are, E HOMO , E LUMO , energy of the gap (E), charge on the reactive center, dipole moments and global hardness. Both experimental and theoretical investigations prove that 4-phenyl-thiosemicarbazide can inhibit better than 4-allyl-thiosemicarbazide. SEM and EDX examination of the C-steel in 2 M HCl surface revealed that these compounds prevented C-steel in 2 M HCl from corrosion by adsorption on its surface to form a protective film and acts as a barrier to corrosive media. Molecular docking was utilized to predict the binding among thiosemicarbazide derivatives with the receipt of breast cancer mutant 3tt8.
A convenient synthesis of a series of pyrimidine, 4 H-3,1-benzoxazin-4-one, pyrazolo[5,1-b]quinaz... more A convenient synthesis of a series of pyrimidine, 4 H-3,1-benzoxazin-4-one, pyrazolo[5,1-b]quinazoline, pyrido[1,2-a]quinazoline, and chromeno[3 ,4 :4,5]pyrido[1,2-a]quinazoline derivatives, via the reactions of versatile and readily accessible methyl 2-(2-cyanoacetamido)benzoate (1) with the appropriate reagents, is described here.
ABSTRACT This review deals with the synthesis and reactions of 5-acetylthiazoles. Some of these r... more ABSTRACT This review deals with the synthesis and reactions of 5-acetylthiazoles. Some of these reactions have been used successfully for the production of biologically important compounds. The main purpose of this review is to present a survey of the literature on the chemistry of 5-acetylthiazoles and to provide useful and up-to-date information on their applications because these compounds have not been previously reviewed. GRAPHICAL ABSTRACT
New series of novel functionalized thiazoles, 1,3,4-thiadiazoles and pyrido[2,3-d][1,2,4]triazolo... more New series of novel functionalized thiazoles, 1,3,4-thiadiazoles and pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidines containing pyrazole moiety were synthesized using 4-acetylpyrazole as a precursor. The structures of the compounds prepared were confirmed by both spectral and elemental analyses and by alternative synthetic routes. The mechanisms of the studied reactions were also discussed. Sixteen compounds were evaluated for their in vitro antimicrobial activity. The results proclaimed that some of the tested compounds exhibited moderate to significant antibacterial and antifungal activities. Compounds 11e, 11a, and 11d exhibited high antibacterial activity against Bacillus subtilis compared with reference drug (Ampicillin) while compounds 11a, 6g, 18e, 18a, 11d, 6a, 11c, 11b and 6d exhibited higher antifungal activity against Syncephalastrum racemosum than reference drug (Amphotericin B).
... A. El-Shafei,1 AA Fadda,2 S. Bondock,2 AM Khalil,2 and Eman H. Tawfik2 1Fiber and Polymer Che... more ... A. El-Shafei,1 AA Fadda,2 S. Bondock,2 AM Khalil,2 and Eman H. Tawfik2 1Fiber and Polymer Chemistry Program, North Carolina State University, Raleigh, North Carolina, USA 2Faculty of Science, Department of Chemistry, Mansoura University, Mansoura, Egypt ...
ChemInform Abstract Die Alkylierung der Heterocyclen (I) und (IV) mit den Alkylbromiden (II) lief... more ChemInform Abstract Die Alkylierung der Heterocyclen (I) und (IV) mit den Alkylbromiden (II) liefert die Ammoniumsalze (III) beziehungsweise (V). Die synthetisierten Verbindungen sind baktericid und fungicid wirksam.
A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzene... more A novel series of 2,4,5- and 2,3,4-trisubstituted thiazole hybrids with 1,3,4-thiadiazolylbenzenesulfonamide was designed following the tail approach as possible hCAIX inhibitors.
Abstract In an attempt to develop active antimicrobial agents, a set of new thiazolyl chalcones h... more Abstract In an attempt to develop active antimicrobial agents, a set of new thiazolyl chalcones has been synthesized by the Claisen–Schmidt reaction of 5-acetyl-4-methyl-2-(3-pyridyl)thiazole with various heterocyclic aldehydes in alkali media. Reaction of chalcones with hydrazine hydrate has resulted in pyrazolines that have been assessed for in vitro antimicrobial activity against ten bacterial and five fungal human pathogenic strains using the disk diffusion assay. The synthesized pyrazolines demonstrate antimicrobial activity higher than that of synthesized chalcones. 2-Thienylchalcone has been determined as the most active against P. aeruginosa . Three pyrazolines are characterized by distinctive activity towards Gram-negative bacteria S. flexneri and P. aeruginosa . Two pyrazolines demonstrate equipotent antifungal activity with amphotricin B against A. clavatus .
Toward finding potential and novel anticancer agents, we designed and prepared novel differently ... more Toward finding potential and novel anticancer agents, we designed and prepared novel differently substituted unsymmetrical azine-modified thiadiazole sulfonamide derivatives using the “combi-targeting approach”.
Lignosulfonate (LS) is a byproduct obtained from the sulfite pulping process, LS improves the phy... more Lignosulfonate (LS) is a byproduct obtained from the sulfite pulping process, LS improves the physical properties of several biopolymer as gelatin. On the other hand, the physicochemical modification of cellulose is a must for making it more applicable in several fields rather than paper or textile industries. Here, we report the fabrication of films derived from calcium lignosulfonate (Ca LS)/sodium cellulose composite for the first time. Which can be used in food packaging to preserve the quality and safety of the food. In order to characterize sodium cellulose and the synthesized composite films, Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM), and thermogravimetric analysis along with water vapor transmission and permeability tests were carried out. The XPS spectrum of sodium cellulose showed a sharp Na (1s) peak (1045 eV), which emphasized the presence of Na + ions. The FT-IR sp...
International Journal of Biological Macromolecules, 2019
N-allylthiourea chitosan (ATUCS), a chelating material, was prepared, characterized, and studied ... more N-allylthiourea chitosan (ATUCS), a chelating material, was prepared, characterized, and studied for the removal of arsenazo III ((As(III)) dye from aqueous solution. Scanning electron microscopy (SEM), energy-dispersive X-ray (EDX), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), and 1 Hand 13 Cnuclear magnetic resonance (NMR) were used to characterize the prepared adsorbent and to investigate the adsorption mechanism. Furthermore, the adsorption behavior of chitosan (CS) and ATUCS were studied under various conditions. The equilibrium adsorbed amount of As(III) onto ATUCS was found to be 116.3 mg/g, compared to 87.3 mg/g with respect to CS. The regeneration of the loaded CS and ATUCS were studied using 1:1 solution of H2O2-H2SO4 and reused with certain change in efficiency after the third cycle. The adsorption process was found to fit well with pseudo-second-order kinetic model. The equilibrium data were better described with the Freundlich isotherm. The monolayer adsorption capacity was found to be 204.08 and 90.90 mg/g for the As (III)/ATUCS and As (III)/CS systems, respectively, at 25 C. The pH of the higher uptake of As (III) onto ATUCS and CS was 4-5 and 8.0, respectively. The results demonstrated improved adsorption of As (III) using ATUCS as compared to the CS.
International Journal of Emerging Trends in Engineering and Development, 2018
The efficiency of two thiosemicarbazide derivatives; 4-phenyl-thiosemicarbazide and 4allyl-thiose... more The efficiency of two thiosemicarbazide derivatives; 4-phenyl-thiosemicarbazide and 4allyl-thiosemicarbazide as corrosion inhibitors against C-steel and its adsorption behavior were investigated in 2 M HCl solution using potentiodynamic polarization, electrochemical impedance spectroscopy (EIS) and electrochemical frequency modulation (EFM) techniques. Results revealed that the inhibition efficiency increased with the inhibitor concentration and also indicate both thiosemicarbazide derivatives act as mixed-type inhibitors. EIS spectra exhibit one capacitive loop and confirm the inhibitive ability. Quantum chemical calculations have been employed for the inhibition efficiency of these thiosemicarbazide derivatives for Csteel in aggressive acidic media by means of density functional theory (DFT) methods B3LYP/6-31g* in gas phase. The calculated quantum chemical parameters correlated to the inhibition efficiency are, E HOMO , E LUMO , energy of the gap (E), charge on the reactive center, dipole moments and global hardness. Both experimental and theoretical investigations prove that 4-phenyl-thiosemicarbazide can inhibit better than 4-allyl-thiosemicarbazide. SEM and EDX examination of the C-steel in 2 M HCl surface revealed that these compounds prevented C-steel in 2 M HCl from corrosion by adsorption on its surface to form a protective film and acts as a barrier to corrosive media. Molecular docking was utilized to predict the binding among thiosemicarbazide derivatives with the receipt of breast cancer mutant 3tt8.
A convenient synthesis of a series of pyrimidine, 4 H-3,1-benzoxazin-4-one, pyrazolo[5,1-b]quinaz... more A convenient synthesis of a series of pyrimidine, 4 H-3,1-benzoxazin-4-one, pyrazolo[5,1-b]quinazoline, pyrido[1,2-a]quinazoline, and chromeno[3 ,4 :4,5]pyrido[1,2-a]quinazoline derivatives, via the reactions of versatile and readily accessible methyl 2-(2-cyanoacetamido)benzoate (1) with the appropriate reagents, is described here.
ABSTRACT This review deals with the synthesis and reactions of 5-acetylthiazoles. Some of these r... more ABSTRACT This review deals with the synthesis and reactions of 5-acetylthiazoles. Some of these reactions have been used successfully for the production of biologically important compounds. The main purpose of this review is to present a survey of the literature on the chemistry of 5-acetylthiazoles and to provide useful and up-to-date information on their applications because these compounds have not been previously reviewed. GRAPHICAL ABSTRACT
New series of novel functionalized thiazoles, 1,3,4-thiadiazoles and pyrido[2,3-d][1,2,4]triazolo... more New series of novel functionalized thiazoles, 1,3,4-thiadiazoles and pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidines containing pyrazole moiety were synthesized using 4-acetylpyrazole as a precursor. The structures of the compounds prepared were confirmed by both spectral and elemental analyses and by alternative synthetic routes. The mechanisms of the studied reactions were also discussed. Sixteen compounds were evaluated for their in vitro antimicrobial activity. The results proclaimed that some of the tested compounds exhibited moderate to significant antibacterial and antifungal activities. Compounds 11e, 11a, and 11d exhibited high antibacterial activity against Bacillus subtilis compared with reference drug (Ampicillin) while compounds 11a, 6g, 18e, 18a, 11d, 6a, 11c, 11b and 6d exhibited higher antifungal activity against Syncephalastrum racemosum than reference drug (Amphotericin B).
... A. El-Shafei,1 AA Fadda,2 S. Bondock,2 AM Khalil,2 and Eman H. Tawfik2 1Fiber and Polymer Che... more ... A. El-Shafei,1 AA Fadda,2 S. Bondock,2 AM Khalil,2 and Eman H. Tawfik2 1Fiber and Polymer Chemistry Program, North Carolina State University, Raleigh, North Carolina, USA 2Faculty of Science, Department of Chemistry, Mansoura University, Mansoura, Egypt ...
ChemInform Abstract Die Alkylierung der Heterocyclen (I) und (IV) mit den Alkylbromiden (II) lief... more ChemInform Abstract Die Alkylierung der Heterocyclen (I) und (IV) mit den Alkylbromiden (II) liefert die Ammoniumsalze (III) beziehungsweise (V). Die synthetisierten Verbindungen sind baktericid und fungicid wirksam.
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