新型苯并呋喃类化合物的设计与合成：作为一类靶向真菌N-肉豆蔻酰基转移酶的新型抗真菌剂。第2部分。
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.
作者信息
Ebiike Hirosato, Masubuchi Miyako, Liu Pingli, Kawasaki Ken-ichi, Morikami Kenji, Sogabe Satoshi, Hayase Michiko, Fujii Toshihiko, Sakata Kiyoaki, Shindoh Hidetoshi, Shiratori Yasuhiko, Aoki Yuko, Ohtsuka Tatsuo, Shimma Nobuo
机构信息
Department of Chemistry, Nippon Roche Research Center, 200 Kajiwara, Kamakura, 247-8530, Kanagawa, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Feb 25;12(4):607-10. doi: 10.1016/s0960-894x(01)00808-3.
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.
对N-肉豆蔻酰基转移酶（Nmt）抑制剂苯并呋喃衍生物6（RO-09-4609）的C-2位进行修饰，使我们发现了在小鼠系统性念珠菌病模型中具有活性的抗真菌剂。药物设计基于对念珠菌Nmt与2形成的复合物晶体结构的分析。优化过程以包括准体内试验和药代动力学分析在内的各种生物学评估为指导。
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