1,2,3-Triazole incorporated coumarin derivatives as potential antifungal and antioxidant agents

作     者：Mubarak H.Shaikh Dnyaneshwar D.Subhedar Firoz A.Kalam Khan Jaiprakash N.Sangshetti Bapurao B.Shingate 

作者机构：Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University Department of Pharmaceutical Chemistry Y. B. Chavan College of Pharmacy Dr. Rafiq Zakaria Campus 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2016年第27卷第2期

页      面：295-301页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 10[医学] 

基　　金：Council of Scientific and Industrial Research  India  CSIR 

主　　题：ADME prediction Antifungal Antioxidant Docking study 1,2,3-Triazole 

摘      要：A series of novel ethyl-7-（（1-（benzyl）-1H-1,2,3-triazol-4-yl）methoxy）-2-oxo-2H-chromene-3-carboxylates 8a-h as potential antifungal agents were synthesized via click chemistry. The antifungal activity was evaluated against five human pathogenic fungal strains, such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger and Cryptococcus neoformans. Compound 8c, 8d, 8e and 8h were found to be equipotent against C. albicans when compared with miconazole and compound 8f was found to be two-fold more active compared with miconazole and equipotent to fluconazole against ***. The coumarin-based triazole derivatives were also evaluated for antioxidant activity and compound 8a was found to be potent antioxidant when compared with standard drug. Furthermore,molecular docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of fungal C. albicans enzyme P450 cytochrome lanosterol 14 ademethylase. Moreover, the synthesized compounds were also analyzed for ADME properties and showed potential to build up as good oral drug candidates.