Abstract

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, ¹H NMR, and MS spectral data. Our new synthesized compounds were screened for in vitro anti-bacterial and anti-fungal activities. It was found that most of the selected compounds exhibited antimicrobial activity especially compounds 3a, b, f which 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 against B. subtilis and 0.8 of Amikacin activity against S. aureus, E. coli, and P. aeruginosa. Concerning the antifungal activity, 3f was 16 times and 4 times more potent than Nystatin against A. niger and C. albicans, respectively. Docking of 3f at the active site of MurA was studied to explore the mode of action of these compounds.

摘要

设计、合成了新系列的芳基吡唑和芳基吡唑并[1,5- a ]嘧啶，并对其抗菌活性进行了评估。新化合物的结构得到 IR、¹ H NMR 和 MS 光谱数据的支持。我们筛选了我们新合成的化合物的体外抗菌和抗真菌活性。发现大多数选定的化合物表现出抗微生物活性，尤其是化合物3a、b、f，与参考药物阿米卡星和制霉菌素相比，它们分别对选定的菌株表现出优异的抗菌和抗真菌活性。关于最有效化合物3f的抗菌活性；它引发了 1.6 倍的阿米卡星活性B. subtilis和 0.8 Amikacin 对 S 的活性。金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌。关于抗真菌活性，3f对黑曲霉和白色念珠菌的效力分别是制霉菌素的 16 倍和 4 倍。研究了3f在 MurA 活性位点的对接，以探索这些化合物的作用方式。