Structure-activity relationships of anti-HIV-1 N-alkoxy- and N-allyloxy-benzimidazoles

被引:57
作者
Evans, TM
Gardiner, JM
Mahmood, N
Smis, M
机构
[1] UNIV MANCHESTER, INST SCI & TECHNOL, DEPT CHEM, MANCHESTER M60 1QD, LANCS, ENGLAND
[2] MRC, CTR COLLABORAT, LONDON NW7 1AD, ENGLAND
关键词
D O I
10.1016/S0960-894X(97)00022-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
One-pot benzimidazole syntheses have been used to prepare an extended series of novel analogues which were evaluated against HIV-1 infectivity, the most active having an EC(50) of 0.5 mu M. There is a correlation between the length of saturated alkyl groups at O1 and C2 with antiviral selectivity. Replacing vinyl by the 2,2-dimethyl vinyl group increases antiviral selectivity. (C) 1997, Elsevier Science Ltd.
引用
收藏
页码:409 / 412
页数:4
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