Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors

…, S Wang, X Che, H Ji, Z Miao, J Yao, W Zhang

Index: Sheng, Chunquan; Xu, Hui; Wang, Wenya; Cao, Yongbing; Dong, Guoqiang; Wang, Shengzheng; Che, Xiaoying; Ji, Haitao; Miao, Zhenyuan; Yao, Jianzhong; Zhang, Wannian European Journal of Medicinal Chemistry, 2010 , vol. 45, # 9 p. 3531 - 3540

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Citation Number: 34

Abstract

N-myristoyltransferase (NMT) has been a promising new target for the design of novel antifungal agents with new mode of action. A series of benzoxazole and indole derivatives were designed and synthesized as isosteric analogues of benzoheterocyclic NMT Inhibitors. In vitro antifungal assay indicated that the benzoxazole derivatives were far more potent than the indoles. Molecular docking studies revealed that the hydrogen bonding ...