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

…, BA Sharpe, RC Lee, JH Griffin, JO Capobianco…

Index: Rose, Ingo C.; Sharpe, Bradley A.; Lee, Roger C.; Griffin, John H.; Capobianco, John O.; Zakula, Dorothy; Goldman, Robert C. Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 1 p. 97 - 103

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Citation Number: 16

Abstract

The design, synthesis and in vitro biological evaluation of pyridinium ion based inhibitors of oxidosqualene cyclase enzymes are reported. N-Alkyl-and 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 ...