Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Molecules. 2021 Apr 15;26(8):2292. doi: 10.3390/molecules26082292.
The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11-15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound is the most potent congener with an MIC value of 2 µg/mL against .
微生物感染的患病率不断上升，以及现有抗菌药物耐药性的出现，促使人们开发具有显著药代动力学和/或药效学特征的新型有效化学实体。因此，设计并合成了一系列新的吲哚-三唑缀合物，通过抑菌圈直径和最低抑菌浓度试验来评估它们作为新型抗菌候选物的潜力，针对某些微生物菌株。它们的体外抗菌评价结果表明，大多数测试的革兰氏阴性菌株对其具有良好至中等的活性，抑菌圈直径（DIZ）值在 11-15 毫米范围内，最小抑菌浓度（MIC）值约为 250μg/mL。同时，它们的体外抗真菌评价结果表明，大多数测试化合物对具有很强的活性，MIC 值低至 2μg/mL。此外，化合物 是最有效的同系物，对 的 MIC 值为 2μg/mL。
