Synthesis of novel HIV-1 protease inhibitors based on carbohydrate scaffolds

被引:47
作者
Murphy, PV [1 ]
O'Brien, JL
Gorey-Feret, LJ
Smith, AB
机构
[1] Natl Univ Ireland Univ Coll Dublin, Dept Chem, Ctr Synth & Chem Biol, Inst Biomol & Biomed Res, Dublin 4, Ireland
[2] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA
[3] Bristol Myers Squibb Co, Wilmington, DE USA
基金
英国惠康基金;
关键词
HIV-1; inhibitors; aspartic acid; carbohydrate based peptidomimetics;
D O I
10.1016/S0040-4020(03)00208-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of peptidomimetic inhibitors of HIV-1 protease based on 6-deoxy-6-aniino-beta-D-glucopyranoside and 6-deoxy-6-amino- beta-D-mannopyranoside scaffolds has been achieved. The inhibitors 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) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2259 / 2271
页数:13
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