Design, Synthesis and Antimicrobial Evaluation of New Arylazopyrazole and Arylazopyrazolo[1,5-a]pyrimidine Derivatives
POLYCYCLIC AROMATIC COMPOUNDS(2022)
摘要
New series of arylazo-pyrazoles and arylazopyrazolo[1,5-a]pyrimidines are designed, synthesized, and evaluated for antimicrobial activity. The structures of new compounds were supported by IR,H-1 NMR, and MS spectral data. Our new synthesized compounds were screened forin vitroanti-bacterial and anti-fungal activities. It was found that most of the selected compounds exhibited antimicrobial activity especially compounds3a, b, fwhich displayed excellent antibacterial and antifungal activities compared to the reference drugs Amikacin and Nystatin, respectively against the selected strains. Regarding antibacterial activity of the most potent compound,3f; it elicited 1.6 folds Amikacin's activity againstB. subtilisand 0.8 of Amikacin activity against S. aureus,E. coli, andP. aeruginosa. Concerning the antifungal activity,3fwas 16 times and 4 times more potent than Nystatin againstA. nigerandC. albicans, respectively. Docking of3fat the active site of MurA was studied to explore the mode of action of these compounds.
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关键词
Antimicrobial activity, docking, pyrazole, pyrazolo[1, 5-a]pyrimidine, synthesis
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