|
|||||
|
|
Inhibition of HIV-1 capsid assembly: Optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold |
|
| Authors: | Martin Tremblay Pierre Bonneau Yves Bousquet Patrick DeRoy Jianmin Duan Martin Duplessis Alexandre Gagnon Michel Garneau Nathalie Goudreau Ingrid Guse Oliver Hucke Stephen H Kawai Christopher T Lemke Stephen W Mason Bruno Simoneau Simon Surprenant Steve Titolo Christiane Yoakim |
| Institution: | 1. Boehringer Ingelheim (Canada) Ltd, Research & Development, Laval, Québec, Canada H7S 2G5;2. Université du Québec à Montréal, Département de Chimie, C.P. 8888, Succ. Centre-Ville, Montréal, Québec, Canada H3C 3P8;3. Bristol-Myers Squibb, Virology, 5 Research Parkway, Wallingford, CT 06492, USA |
| Abstract: | A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved the antiviral potency by a . The X-ray structure of 33 complexed with the capsid N-terminal domain allowed identification of major interactions between the inhibitor and the protein. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |