Structure-based design and synthesis of HIV-1 protease inhibitors employing β-D-mannopyranoside scaffolds

被引：19

作者：

Murphy, PV ^{[1
]}

O'Brien, JL

Gorey-Feret, LJ

Smith, AB

机构：

[1] Univ Coll Dublin, Dept Chem, Ctr Synth & Chem Biol, Conway Inst Biomol & Biomed Res, Dublin 4, Ireland

[2] Bristol Myers Squibb Pharmaceut Co, Wilmington, DE USA

[3] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(02)00220-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A preliminary account on the structure-based design, synthesis and evaluation of peptidomimetic inhibitors of HIV-1 protease containing beta-D-mannopyranoside scaffolds is given. The compounds prepared had IC50 values in the micromolar range. The results provide a platform for the development of more potent carbohydrate-based inhibitors of HIV-1 and other aspartic proteases. (C) 2002 Published by Elsevier Science Ltd.

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收藏

页码：1763 / 1766

页数：4

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