Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase

被引：54

作者：

Tillekeratne, LMV

Sherette, A

Grossman, P

Hupe, L

Hupe, D

Hudson, RA

机构：

[1] Univ Toledo, Coll Pharm, Dept Med & Biol Chem, Toledo, OH 43606 USA

[2] Pfizer Global Res & Dev, Ann Arbor, MI 48105 USA

[3] Univ Toledo, Coll Arts & Sci, Dept Biol, Toledo, OH 43606 USA

[4] Univ Toledo, Coll Arts & Sci, Dept Chem, Toledo, OH 43606 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)00577-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Systematic simplification of the molecular structures of epicatechin gallate and epigallocatechin gallate to determine the minimum structural characteristics necessary for HIV-1 reverse transcriptase inhibition in vitro resulted in several compounds that strongly inhibited the native as well as the A17 double mutant (KI03N Y181C) enzyme, which is normally insensitive to most known nonnucleoside inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2763 / 2767

页数：5

共 24 条

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