Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates

Molecules

卷:26

NadineM. S. Moubayed¹  MahaS. Al-Mutairi²  MohamedI. Attia²  ReemI. Al-Wabli²  MonaA. Alsulami²  SarahI. Bukhari³ 

[1] Botany and Microbiology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia;

[2] Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;

[3] Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia;

关键词: indole;    1,2,4-triazole-3-thiol;    antibacterial;    antifungal;   

DOI  :  10.3390/molecules26082292

来源: DOAJ

【 摘 要 】

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 6a-u 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 Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans.

【 授权许可】

Unknown