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

2005; Elsevier BV; Volume: 13; Issue: 7 Linguagem: Inglês

10.1016/j.bmc.2005.01.033

1464-3391

Kazuto Yamazaki, Yasushi Kaneko, Kie Suwa, Shinji Ebara, Kyoko Nakazawa, Kazuhiro Yasuno,

Enzyme function and inhibition

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.