Novel nevirapine-like inhibitors with improved activity against NNRTI-resistant HIV:: 8-heteroarylthiomethyidipyridodiazepinone derivatives

被引:31
作者
Yoakim, C
Bonneau, PR
Déziel, R
Doyon, L
Duan, J
Guse, I
Landry, S
Malenfant, E
Naud, J
Ogilvie, WW
O'Meara, JA
Plante, R
Simoneau, B
Thavonekham, B
Bös, M
Cordingley, MG
机构
[1] Boehringer Ingelheim Canada Ltd, Dept Chem, Res & Dev, Laval, PQ H7S 2GS, Canada
[2] Boehringer Ingelheim Canada Ltd, Res & Dev, Dept Biol Sci, Laval, PQ H7S 2G5, Canada
关键词
D O I
10.1016/j.bmcl.2003.11.049
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 8-heteroarylthiomethyidipyridodiazepinone derivatives were prepared and evaluated for their antiviral profile against wild type virus and the important K103N/Y181C mutant as an indicator for broad activity. 2,6-Dimethylpyridine derivative 16 was found to have a good pharmacokinetic profile in spite of poor metabolic stability in rat liver microsomes. (C) 2003 Published by Elsevier Ltd.
引用
收藏
页码:739 / 742
页数:4
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