Synthesis and antifungal activities of some thiolane-triazole derivatives.
As part of our search for active agents against systemic fungal infections, a new series of triazole compounds with a thiolane ring was synthesized. Their antifungal activities were investigated in vitro and in vivo. Some of these thiolanetriazoles showed promising activity, comparable to that of ketoconazole, against a mouse systemic Candida albicans infection, after oral or parenteral dosing.
Konosu
T
T
Medical Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Takeda
N
N
Tajima
Y
Y
Yasuda
H
H
Oida
S
S
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis*; D002177:Candidiasis / Q000188:drug therapy / Q000382:microbiology; D055598:Chemical Phenomena; D002621:Chemistry; D005658:Fungi / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000935:Antifungal Agents; D013438:Sulfhydryl Compounds; D014230:Triazoles