Design and Synthesis of Stereochemically Defined Novel Spirocyclic P2-Ligands for HIV-1 Protease Inhibitors
Design and Synthesis of Stereochemically Defined Novel Spirocyclic P2-Ligands for HIV-1 Protease Inhibitors
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DOI：
10.1021/ol8020308
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发表时间：
2008-11-20
期刊：
影响因子：
5.2
通讯作者：
Mitsuya, Hiroaki
中科院分区：
文献类型：
--
作者：
Ghosh, Arun K.;Chapsal, Bruno D.;Mitsuya, Hiroaki
描述了一系列立体化学定义的螺环化合物的合成及其作为 HIV-1 蛋白酶抑制剂的新型 P2 配体的用途。配体的双环核心是通过有效的 nBu(3)SnH 促进的 1,6-烯炔自由基环化然后氧化裂解来合成的。报道了基于结构的设计、配体的合成以及所得抑制剂的生物学评价。
The synthesis of a series of stereochemically defined spirocyclic compounds and their use as novel P2-ligands for HIV-1 protease inhibitors are described. The bicyclic core of the ligands was synthesized by an efficient nBu(3)SnH-promoted radical cyclization of a 1,6-enyne followed by oxidative cleavage. Structure-based design, synthesis of ligands, and biological evaluations of the resulting inhibitors are reported.