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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3 |
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| Authors: | Kawasaki Ken-ichi Masubuchi Miyako Morikami Kenji Sogabe Satoshi Aoyama Tsunehisa Ebiike Hirosato Niizuma Satoshi Hayase Michiko Fujii Toshihiko Sakata Kiyoaki Shindoh Hidetoshi Shiratori Yasuhiko Aoki Yuko Ohtsuka Tatsuo Shimma Nobuo |
| Institution: | Department of Chemistry, Nippon Roche Research Center, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan. |
| Abstract: | 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. |
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