3-Iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

被引:33
作者
Benjahad, A
Guillemont, J
Andries, K
Nguyen, CH
Grierson, DS
机构
[1] Inst Curie, UMR 176 CNRS, Lab Pharmacochim, Sect Rech, F-91405 Orsay, France
[2] Johnson & Johnson Pharmaceut Res & Dev, Virol Drug Discovery, B-2340 Beerse, Belgium
[3] Johnson & Johnson Pharmaceut Res & Dev, Dept Med Chem, Val De Reuil, France
关键词
D O I
10.1016/j.bmcl.2003.09.045
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Building upon the potent anti-HIV-1 activities observed for the 3-dimethylamino-4-benzylpyridinone 2, and the corresponding 4-aryloxypyridinone analogue 3, a concise and efficient route to the 3-iodo-4-aryloxypyridinones 14a-c (IOPY's) was developed. This involved reaction of the 4-hydroxy substituted pyridinone 10 with the requisite dichloroiodobenzene reagent 11. IOPY compound 14c is active at IC50 = 1-45 nM against wild type HIV-1 and a panel of six major simple/double HIV mutant strains. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4309 / 4312
页数:4
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