Research Interests:
... Acknowledgments The authors are grateful to Prof. Dr. Nabil A. Monsour and Dr. MahmoudMorshedy, Faculty of Agriculture, University of Alexan-dria, for providing laboratory facilities and for their kind help. Journal of Pharmaceutical... more
... Acknowledgments The authors are grateful to Prof. Dr. Nabil A. Monsour and Dr. MahmoudMorshedy, Faculty of Agriculture, University of Alexan-dria, for providing laboratory facilities and for their kind help. Journal of Pharmaceutical Sciences / 833 Vol. 76, No. ...
Research Interests:
Three main classes of quinoxaline derivatives have been synthesized. The first class comprises the synthesis of three novel series of 1,2,4-triazolo[4,3-a]quinoxalines; namely 1-substituted-1,2,4-triazolo[4,3-a]quinoxalines 3a-f,... more
Three main classes of quinoxaline derivatives have been synthesized. The first class comprises the synthesis of three novel series of 1,2,4-triazolo[4,3-a]quinoxalines; namely 1-substituted-1,2,4-triazolo[4,3-a]quinoxalines 3a-f, 1-substituted aminomethyl-1,2,4-triazolo[4,3-a]quinoxalines 14a-d and 1-cyano or ethoxycarbonylmethyl-1,2,4-triazolo[4,3-a]quinoxalines 6, 12. The second class involves the synthesis of 2-substituted-1 H-1,2,4-triazino[4,3-a]quinoxalines 4a-d. The third class deals with the synthesis of a variety of 2-pyrazolylquinoxalines, namely 2-(5-amino-3-arylpyrazol-1-yl)-3-phenylquinoxalines 5a-d, 2-[5-hydroxy-3-phenyl-4-(4-substituted sulfamoylphenyl)azopyrazol-1-yl]-3-phenylquinoxalines 15a, b, and 2-(5-hydroxy-4-nitroso-3-phenylpyrazol-1-yl)-3-phenylquinoxalin e (16). The prepared compounds were tested in vitro for their antimicrobial activity. Compounds 13 and 14b exhibited promising antifungal activity against C. albicans (MIC 25, 50 mu/ml respectively). Compound 13 was as active as the antibiotic nystatin.
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Development of new antimicrobial agents is a good solution to overcome drug-resistance problems. From this perspective, new quinoxaline derivatives bearing various bioactive heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and... more
Development of new antimicrobial agents is a good solution to overcome drug-resistance
problems. From this perspective, new quinoxaline derivatives bearing various bioactive
heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and thiazoles) were designed and
synthesized. The newly synthesized compounds were evaluated for their in-vitro
antibacterial activity against nine bacterial human pathogenic strains using the disc diffusion
assay. In general, most of the synthesized compounds exhibited good antibacterial activities.
The thiazolyl 11c displayed significant antibacterial activities against P. aeruginosa (MIC,
12.5 μg/mL vs levofloxacin 12.5μg/mL).Molecular docking studies indicated that the
synthesized compounds could occupy both p-amino benzoic acid (PABA) and pterin binding
pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could
act by the inhibition of bacterial DHPS enzyme. The results provide important information
for the future design of more potent antibacterial agents.
problems. From this perspective, new quinoxaline derivatives bearing various bioactive
heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and thiazoles) were designed and
synthesized. The newly synthesized compounds were evaluated for their in-vitro
antibacterial activity against nine bacterial human pathogenic strains using the disc diffusion
assay. In general, most of the synthesized compounds exhibited good antibacterial activities.
The thiazolyl 11c displayed significant antibacterial activities against P. aeruginosa (MIC,
12.5 μg/mL vs levofloxacin 12.5μg/mL).Molecular docking studies indicated that the
synthesized compounds could occupy both p-amino benzoic acid (PABA) and pterin binding
pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could
act by the inhibition of bacterial DHPS enzyme. The results provide important information
for the future design of more potent antibacterial agents.