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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3

2003; Elsevier BV; Volume: 13; Issue: 1 Linguagem: Inglês

10.1016/s0960-894x(02)00844-2

1464-3405

Ken‐ichi Kawasaki, Miyako Masubuchi, Kenji Morikami, Satoshi Sogabe, Tsunehisa Aoyama, Hirosato Ebiike, Satoshi Niizuma, Michiko Hayase, Toshihiko Fujii, Kiyoaki Sakata, Hidetoshi Shindoh, Yasuhiko Shiratori, Yuko Aoki, Tatsuo Ohtsuka, Nobuo Shimma,

Cancer therapeutics and mechanisms

A new series of acid-stable antifungal agents having strong inhibitory activity against Candida albicans N-myristoyltransferase (CaNmt) has been developed starting from acid-unstable benzofuranylmethyl aryl ether 2. The inhibitor design is based on X-ray crystallographic analysis of a CaNmt complex with aryl ether 3. Among the new inhibitors, pyridine derivative 8b and benzimidazole derivative 8k showed clear antifungal activity in a murine systemic candidiasis model.