Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors

被引：19

作者：

Baker, CT ^{[1
]}

Salituro, FG ^{[1
]}

Court, JJ ^{[1
]}

Deininger, DD ^{[1
]}

Kim, EE ^{[1
]}

Li, BQ ^{[1
]}

Novak, PM ^{[1
]}

Rao, BG ^{[1
]}

Pazhanisamy, S ^{[1
]}

Schairer, WC ^{[1
]}

Tung, RD ^{[1
]}

机构：

[1] Vertex Pharmaceut Inc, Cambridge, MA 02139 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(98)00669-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors bearing a structurally novel backbone. Detailed structural analysis of several inhibitors prepared in this series has suggested that rigidification of the P-1/P-2 region of this class of molecules may result in compounds with improved potency. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：3631 / 3636

页数：6

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