N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action

被引:41
作者
Lagoja, IM
Pannecouque, C
Van Aerschot, A
Witvrouw, M
Debyser, Z
Balzarini, J
Herdewijn, P
De Clercq, E
机构
[1] Katholieke Univ Leuven, Rega Inst Med Res, Med Chem Lab, B-3000 Louvain, Belgium
[2] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium
关键词
D O I
10.1021/jm0211117
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of N-aminoimidazoles (NAIMs) with an uncommon spectrum of antiretroviral activity is described. From a group of 60 closely related molecules, we were able to subdivide the molecules in different groups based on their anti-HIV and anti-SIV activity in vitro (i) molecules acting on a new, immediate postintegration step, (ii) molecules acting on both postintegration and HIV-1 reverse transcriptase (RT) as NNRTI, and (iii) molecules that mainly act at the HIV-1 RT according to an NNRTI-type mode of action.
引用
收藏
页码:1546 / 1553
页数:8
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