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

页码：3402 / 3406

页数：5

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