[Synthesis and antifungal activity of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols].
Twenty-three 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols were synthesized and evaluated for antifungal activities in vitro. The synthetic methods of the intermediates are also reported. The compounds belong to two kinds: sulfones and sulfides. All of the compounds are new. The results of preliminary antifungal test showed that most of the sulfide derivatives exhibited potent activities against six kinds of common pathogenic fungi such as Microsporum lanosum, Cryptococcus neoformans, Candida albicans, Aspergillus fumigatus, Cladosporium carrionii, and Saccharomyces torulopsis in vitro. Compounds IVe, f,i,j showed equal or more potent activities when compared with ketoconazole and were markedly superior to fluconazole. The sulfone derivatives showed lower antifungal activity.
Zhang
D Z
DZ
College of Pharmacy, Second Military Medical University, Shanghai 200433.
Zhou
T S
TS
Wu
Y J
YJ
Liu
C M
CM
Ma
M C
MC
Feng
X T
XT
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D015725:Fluconazole / Q000494:pharmacology; D007654:Ketoconazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008864:Microsporum / Q000187:drug effects; D012440:Saccharomyces / Q000187:drug effects; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000935:Antifungal Agents; D014230:Triazoles; D015725:Fluconazole; D007654:Ketoconazole