Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase.: Part 2
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase.: Part 2
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DOI：
10.1016/s0960-894x(01)00808-3
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发表时间：
2002-02-25
影响因子：
2.7
通讯作者：
Shimma, N
中科院分区：
文献类型：
--
作者：
Ebiike, H;Masubuchi, M;Shimma, N
对N-肉豆蔻酰转移酶(NMT)抑制剂苯并呋喃衍生物6(RO-09-4609)C-2位的修饰使我们发现了在小鼠系统性念珠菌病模型中有效的抗真菌药物。药物设计是基于对假丝酵母菌NMT与2的晶体结构的分析。优化得到了各种生物学评价的指导，包括准体内试验和药代动力学分析。(C)2002爱思唯尔科学有限公司。保留所有权利。
Modification of the C-2 position of a benzofuran derivative 6 (RO-09-4609), an N-myristoyltransferase (Nmt) inhibitor, has led us to discover antifungal agents that are active in a murine systemic candidiasis model. The drug design is based on the analysis of a crystal structure of a Candida Nmt complex with 2. The optimization has been guided by various biological evaluations including a quasi in vivo assay and pharmacokinetic analysis. (C) 2002 Elsevier Science Ltd. All rights reserved.