[Synthesis of novel antifungal triazoles and study on their activity].
OBJECTIVE
Design, synthesis and activity study of novel antifungal triazoles.


METHODS
The structures of two lead-compounds miconazole and itrconazole were modified on the basis of SAR studied by our group and reported in the literature and their antifungal activities in vitro were tested by standard program.


RESULTS
Twelve 1-(1H-1, 2, 4-triazole-1-yl) -2-( 2, 4-difluorophenyl)-3-substituted amino-2-propanol compounds and thirteen 2-substituted phenyl-5-(1H-1, 2, 4-triazole-1-methyl ) 5-( 2, 4-difluorophenyl)-N-substituted oxazolidine compounds were synthesized and confirmed by 1HNMR and MS. In vitro inhibitory tests showed that most of them have more or less inhibitory effects on C. albicans and some inhibit S. cerevisiae also. Especially the effects of A10, A12 and A13 on C. albicans were more potent than (or equal to) that of fluconazole or itraconazole.


CONCLUSIONS
Compounds A10, A12 and A13 are worthy to be intensively studied.
Chu
Yong
Y
Pharmacy School of West China, Sichuan University, Chengdu 610041, China. dr.ychu@163.com
Xu
Ming-Xia
MX
Lü
Ding
D
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001234:Aspergillus niger / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects*; D003455:Cryptococcus neoformans / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000935:Antifungal Agents; D014230:Triazoles