NOVEL HIV-1 PROTEASE INHIBITORS CONTAINING A BETA-HYDROXY SULFIDE ISOSTERE

被引:6
作者
CHO, SYS [1 ]
JUNGHEIM, LN [1 ]
BAXTER, AJ [1 ]
机构
[1] ELI LILLY & CO,LILLY RES LAB,INDIANAPOLIS,IN 46285
关键词
D O I
10.1016/S0960-894X(01)80186-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of analogues of LY289612 were prepared as HIV-1 protease inhibitors and evaluated in vitro for their enzyme inhibitory and antiviral activities. Compound 1, a potent HIV-1 protease inhibitor, and its analogues were synthesized from key intermediate 9, which was prepared by alkylation of mercaptan 4 with alpha-bromo ketone 7 followed by stereoselective reduction of the ketone intermediate 8.
引用
收藏
页码:715 / 720
页数:6
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