Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1

…, S Tsujii, S Sogabe, T Fujii, K Sakata, Y Shiratori…

Index: Masubuchi, Miyako; Kawasaki, Ken-ichi; Ebiike, Hirosato; Ikeda, Yoshihiko; Tsujii, Shinji; Sogabe, Satoshi; Fujii, Toshihiko; Sakata, Kiyoaki; Shiratori, Yasuhiko; Aoki, Yuko; Ohtsuka, Tatsuo; Shimma, Nobuo Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 14 p. 1833 - 1837

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Citation Number: 89

Abstract

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitors have been identified through optimization of a lead compound 1 discovered by random screening. The inhibitor design is based on the crystal structure of the CaNmt complex with compound (S)-3 and structure–activity relationships (SARs) have been clarified. Modification of the C-4 side chain of 1 has led to the discovery of a potent and selective CaNmt inhibitor 11 (RO-09- ...