Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands

被引：8

作者：

Chen, XQ ^{[1
]}

Kempf, DJ ^{[1
]}

Sham, HL ^{[1
]}

Green, BE ^{[1
]}

Molla, A ^{[1
]}

Korneyeva, M ^{[1
]}

Vasavanonda, S ^{[1
]}

Wideburg, NE ^{[1
]}

Saldivar, A ^{[1
]}

Marsh, KC ^{[1
]}

McDonald, E ^{[1
]}

Norbeck, DW ^{[1
]}

机构：

[1] Abbott Labs, Div Pharmaceut Prod, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(98)00653-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 2-isopropyl thiazolyl group is a highly optimized P-3 ligand for C-2 symmetry-based HIV protease inhibitors, as exemplified in the drug ritonavir. Here we report that incorporation of this P-3 ligand into a piperazine hydroxyethylamine series also yielded novel, highly potent inhibitors. In tissue culture assays, the presence of human serum was less deleterious to the activity of these inhibitors than to that of ritonavir. Furthermore, potent activity against ritonavir resistant HIV was observed. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3531 / 3536

页数：6

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