Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant

被引：85

作者：

Muraglia, E

Kinzel, OD

Laufer, R

Miller, MD

Moyer, G

Munshi, V

Orvieto, F

Palumbi, MC

Pescatore, G

Rowley, M

Williarns, PD

Summa, V

机构：

[1] MRL Rome, IRBM, Dept Med Chem, I-00040 Rome, Italy

[2] MRL Rome, IRBM, Dept Pharmacol, I-00040 Rome, Italy

[3] WP MRL, Dept Antiviral Res, West Point, PA 19486 USA

[4] WP MRL, Dept Med Chem, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

HIV; non-nucleoside reverse transcriptase inhibitors; tetrazole thioacetanilides;

D O I：

10.1016/j.bmcl.2006.02.024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats. (C) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2748 / 2752

页数：5

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