4-Hydroxy-5,6-dihydro-2H-pyran-2-ones.: 3.: Bicyclic and heteroaromatic ring systems as 3-position scaffolds to bind to S1′ and S2′ of the HIV-1 protease enzyme.

被引：8

作者：

Ellsworth, EL

Domagala, J

Prasad, JVNV

Hagen, S

Ferguson, D

Holler, T

Hupe, D

Graham, N

Nouhan, C

Tummino, PJ

Zeikus, G

Lunney, EA

机构：

[1] Warner Lambert Co, Parke Davis Pharmaceut Res Div, Dept Chem, Ann Arbor, MI 48105 USA

[2] Warner Lambert Co, Parke Davis Pharmaceut Res Div, Dept Biochem, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00332-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5,6-Dihydro-2H-pyran-2-ones are potent inhibitors of HIV-1 protease, which bind to the S-1, S-2, S-1', and S-2' pockets and have a unique binding mode with the catalytic aspartyl groups and the flap region of the enzyme. Efforts to explore 3-position heterocyclic scaffolds that bind to the S-1' and S-2' pockets have provided a number of selected analogs that display high HIV-1 protease inhibitory activity, (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2019 / 2024

页数：6

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