✦ LIBER ✦

Design, synthesis and in vitro evaluation of pyridinium ion based cyclase inhibitors and antifungal agents

✍ Scribed by Ingo C. Rose; Bradley A. Sharpe; Roger C. Lee; John H. Griffin; John O. Capobianco; Dorothy Zakula; Robert C. Goldman

Book ID: 103992196
Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 619 KB
Volume: 4
Category: Article
ISSN: 0968-0896
DOI: 10.1016/0968-0896(95)00177-8

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✦ Synopsis

The design, synthesis and in vitro biological evaluation of pyridinium ion based inhibitors of oxidosqualene cyclase enzymes are reported. N-Alkyland N-prenylpyridinium ions have been found to be potent and specific inhibitors of Candida albicans oxidosqualene-lanosterol cyclase and to exhibit antifungal activity. The ability of pyridinium ions to inhibit the C. albicans cyclase increases with increasing structural resemblance to a putative monocyclized species formed during the course of the cyclization process. The N-(4E,8E)-5,9,13-trimethyl-4,8,12-tetradecatrien-l-ylpyridinium cation 1 inhibits the C. albicans enzyme at concentrations more than 100-fold lower than does the directly analogous piperidinium derivative 4.

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