Triazole Antifungals. II

Triazole compounds with an oxazolidine ring were designed and synthesized as a potential inhibitor of the fungal cytochrome P450 14α-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (4R, 5R)-3-acyl-4-methyloxazolidine derivatives 4 exhibited remark...

Full description

Saved in:
Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 38; no. 9; p. 2476
Main Authors KONOSU, Toshiyuki, TAJIMA, Yawara, TAKEDA, Noriko, MIYAOKA, Takeo, KASAHARA, Mayumi, YASUDA, Hiroshi, OIDA, Sadao
Format Journal Article
LanguageEnglish
Published Tokyo Japan Science and Technology Agency 01.09.1990
Online AccessGet full text

Cover

More Information
Summary:Triazole compounds with an oxazolidine ring were designed and synthesized as a potential inhibitor of the fungal cytochrome P450 14α-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (4R, 5R)-3-acyl-4-methyloxazolidine derivatives 4 exhibited remarkably high efficacy after oral or parenteral dosing. The potent activity of 4 is hypothesized to be a consequence of a structural similarity between 4 and lanosterol, a target molecule of the cytochrome P450 14α-demethylase. Highly stereoselective synthesis of these oxazolidines is also described.
ISSN:0009-2363
1347-5223