Design, synthesis and antifungal activity of novel triazoles containing propyl side chains
10.12206/j.issn.2097-2024.202208016
- VernacularTitle:含丙基侧链的新型三唑类化合物的设计、合成和抗真菌活性研究
- Author:
Haidong ZHANG
1
;
Fumiao YUAN
1
;
Dazhi ZHANG
1
;
Yuanying JIANG
2
;
Shichong YU
1
Author Information
1. School of Pharmacy, Naval Medical University, Shanghai 200433, China.
2. School of Pharmacy, Naval Medical University, Shanghai 200433, China;Medical College, Tongji University, Shanghai 200092, China.
- Keywords:
triazole derivatives;
N-propyl side chain;
disubstituted benzyl group;
synthesis;
antifungal activity
- From:
Journal of Pharmaceutical Practice
2023;41(2):86-90
- CountryChina
- Language:Chinese
-
Abstract:
Objective To study the antifungal activity of a new series of triazole compounds with n-propyl side chain and disubstituted benzyl structure. Methods Eleven target compounds were designed and synthesized. The structures were confirmed by 1H NMR, and some compounds were confirmed by 13C NMR or HRMS. Three fungal strains were selected as experimental strains, and the antifungal activity was tested in vitro according to the standardized antifungal sensitivity test method recommended by National Committee for Clinical Laboratory Standards (NCCLS). Results Compound B11 showed better activity against candida albicans SC5314 than fluconazole and was comparable to posaconazole; Compounds B10, B11 and B4 showed better activity against cryptococcus neoformanis H99 than fluconazole, while compounds B2, B3, B5, B6 and B7 showed similar activity to fluconazole against cryptococcus neoformanis H99; while all compounds showed poor activity against aspergillus fumigatus. Conclusion Some of the target compounds with n-propyl side chain and disubstituted benzyl group structure had certain antifungal activity and could be identified as potential lead antifungal drugs.
