Synthesis of potent C2-symmetric, diol-based HIV-1 protease inhibitors.: Investigation of thioalkyl and thioaryl P1/P1′ substituents

被引：17
|
作者：
Mühlman, A
Classon, B
Hallberg, A
Samuelsson, B [1 ]
机构：
[1] Stockholm Univ, Dept Organ Chem, Arrhenius Lab, SE-10691 Stockholm, Sweden
[2] Uppsala Univ, Dept Organ Pharmaceut Chem, BMC, SE-75123 Uppsala, Sweden
[3] Medivir AB, SE-14144 Huddinge, Sweden
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 21期
关键词：
D O I：
10.1021/jm0011169
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of novel, potent diol-based HIV-1 protease inhibitors, having either -SAr, -SCH2-Ar, or -SCH2R groups as P1/P1' substituents is described. They can be prepared using a straightforward synthesis involving a thiol nucleophilic ring opening of a diepoxide. Inhibitor 13 was found to be a potent inhibitor of HIV-1 PR, showing good antiviral activity in a cell-based assay.
引用
收藏
页码：3402 / 3406
页数：5
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