Evaluation of furofuran as a P-2 ligand for symmetry-based HIV protease inhibitors

被引：10

作者：

Chen, XQ

Li, L

Kempf, DJ

Sham, H

Wideburg, NE

Saldivar, A

Vasavanonda, S

Marsh, KC

McDonald, E

Norbeck, DW

机构：

[1] Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, D-47D, AP9A

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(96)00528-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The hexahydrofurofuranyloxy group was evaluated as a conformationally constrained Pt ligand for symmetry-based HIV protease inhibitors. A number of compounds showed nM level activity against HIV in MT4 cells and lower protein binding than the licensed protease inhibitor ritonavir. However, replacement of 5-thiazole of ritonavir with a furofuran caused a reduction of the bioavailability in vivo. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2847 / 2852

页数：6

共 19 条

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