Design and synthesis of novel antifungal compounds bearing quinoline and thiophene moieties
10.3969/j.issn.1006-0111.2017.01.005
- VernacularTitle:新型含喹啉和噻吩结构的抗真菌化合物的设计与合成
- Author:
Lei PANG
1
;
Jing ZHAO
;
Tingjunhong NI
;
Chengxu ZANG
;
Zichao DING
;
Dazhi ZHANG
;
Yuanying JIANG
Author Information
1. 福建中医药大学药学院
- Keywords:
quinoline;
antifungal;
thiophene;
synthesis;
Candida albicans
- From:
Journal of Pharmaceutical Practice
2017;35(1):17-21,86
- CountryChina
- Language:Chinese
-
Abstract:
Objective Based on the structure-activity relationships on the reported antifungal agents bearing quinoline or thiophene moieties ,novel compounds bearing both quinoline and thiophene were designed ,synthesized ,and evaluated for in vitro antifungal activity against Candida albicans .Methods With 5-cyanothiophene-2-carbaldehyde or 5-cyanothiophene-3-car-baldehyde as starting materials ,13 compounds were synthesized via reductive amination ,reduction of cyano group and amida-tion of quinoline-or isoquinoline-carboxylic acid .Their chemical structures were characterized by 1 H NMR and MS . In vitro antifungal screening against Candida albicans SC5314 was performed with the microbroth dilution method .Results All the compounds exhibited potent antifungal activities against Candida albicans .Among them ,compound 6k showed the highest an-tifungal activity with MIC80 value of 0 .5 μg/ml ,which is same potent as fluconazole .Conclusion The designed compounds bearing both quinoline and thiophene exhibited potent antifungal activities ,and deserve further research .
