Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure

…, Y Kaneko, K Suwa, S Ebara, K Nakazawa…

Index: Yamazaki, Kazuo; Kaneko, Yasushi; Suwa, Kie; Ebara, Shinji; Nakazawa, Kyoko; Yasuno, Kazuhiro Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 7 p. 2509 - 2522

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Citation Number: 71

Abstract

Two parallel synthetic methods using solid-supported reagents were established to examine the rapid optimization of weak hit compound 1. Several compounds showed high potency in the low nanomolar range against N-myristoyltransferase. The structure–activity relationship (SAR) and antifungal activities of a series of novel 2-aminobenzothiazole N- myristoyltransferase inhibitors are presented.