Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase

…, K Kawasaki, S Sogabe, K Morikami, Y Shiratori…

Index: Masubuchi, Miyako; Ebiike, Hirosato; Kawasaki, Ken-Ichi; Sogabe, Satoshi; Morikami, Kenji; Shiratori, Yasuhiko; Tsujii, Shinji; Fujii, Toshihiko; Sakata, Kiyoaki; Hayase, Michiko; Shindoh, Hidetoshi; Aoki, Yuko; Ohtsuka, Tatsuo; Shimma, Nobuo Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 20 p. 4463 - 4478

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Citation Number: 101

Abstract

The C-4 side chain modification of lead compound 1 has resulted in the identification of a potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor RO-09- 4609, which exhibits antifungal activity against C. albicans in vitro. Further modification of its C-2 substituent has led to the discovery of RO-09-4879, which exhibits antifungal activity in vivo. The drug design is based on X-ray crystal analysis of a CaNmt complex with ...