Crucial amides for dimerization inhibitors of HIV-1 protease

被引:10
作者
Bowman, MJ [1 ]
Chmielewski, J [1 ]
机构
[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
基金
美国国家卫生研究院;
关键词
D O I
10.1016/j.bmcl.2003.09.099
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An inhibitor based on crosslinked peptides from the interfacial region of HIV-1 protease, previously shown to act by dimerization inhibition, was modified by N-methylation to ascertain the importance of the amide hydrogens on inhibition. The effects of N-methylation on HIV-1 protease inhibition, as well as the effects on degradation by proteases are described. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1395 / 1398
页数:4
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