Synthesis and antifungal activity of 1-(1,2,4-triazolyl-1H-1-yl)-2-(2,4-diflurophenyl)-3-(4-substituted benzyl-1-piperazinyl)-2-propanols.
- Author:
Chun-quan SHENG
1
;
Wan-nian ZHANG
;
Hai-tao JI
;
Yun-long SONG
;
Song YANG
;
You-jun ZHOU
;
Ju ZHU
;
Jia-guo LÜ
Author Information
- Publication Type:Journal Article
- MeSH: Antifungal Agents; chemical synthesis; chemistry; pharmacology; Aspergillus fumigatus; drug effects; Candida albicans; drug effects; Cryptococcus neoformans; drug effects; Microbial Sensitivity Tests; Molecular Structure; Triazoles; chemical synthesis; chemistry; pharmacology
- From: Acta Pharmaceutica Sinica 2003;38(9):665-670
- CountryChina
- Language:Chinese
-
Abstract:
AIMA series of triazole antifungals were synthesized to search for novel triazole antifungals with more potent activity, less toxicity and broader spectrum.
METHODSNineteen 1-(1,2,4-triazolyl-1H-1-yl)-2-(2,4-diflurophenyl)-3-(4-substituted benzyl-1-piperazinyl)-2-propanols were designed and synthesized, on basis of the three dimensional structure of P450 cytochrome 14 alpha-sterol demethylase (CYP51) and their antifungal activities were also evaluated.
RESULTSAll the title compounds were first reported. Results of preliminary biological tests showed that most of the title compounds exhibited high activity against the eight common pathogenic fungi and the activities against deep fungi were higher than that against shallow fungi.
CONCLUSIONMost of the title compounds showed higher antifungal activities than Fluconazole and Terbinafine. Compound VIII-1, 10, 12, 17 showed best antifungal activity with broad antifungal spectrum and were chosen for further development.
