ChemInform Abstract: Synthesis and Antifungal Activity of Novel Thiazole-Containing Triazole Antifungals.

✍ Scribed by A. TSURUOKA; Y. KAKU; H. KAKINUMA; I. TSUKADA; M. YANAGISAWA; T. NAITO

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 35 KB
• Volume: 28
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199751149

✦ Synopsis

Synthesis and Antifungal Activity of Novel Thiazole-Containing Triazole Antifungals.

-A series of new thiazole-containing triazole (IV), (X), (XI), and (XII) antifungals is synthesized on a route shown for the derivatives (IV). A detailed structure-activity relationship study is presented to elucidate the influence of constitution and bulkiness of substituents on the antifungal activity. The most promising results are obtained for derivative (IVd). Moreover, an enantioselective synthesis of the more potent (R)-isomer of (IVd) utilizing Sharpless asymmetric dihydroxylation as the key step is given. -(TSURUOKA, A.;