1421455-12-0Relevant articles and documents
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
Tremblay, Martin,Bonneau, Pierre,Bousquet, Yves,Deroy, Patrick,Duan, Jianmin,Duplessis, Martin,Gagnon, Alexandre,Garneau, Michel,Goudreau, Nathalie,Guse, Ingrid,Hucke, Oliver,Kawai, Stephen H.,Lemke, Christopher T.,Mason, Stephen W.,Simoneau, Bruno,Surprenant, Simon,Titolo, Steve,Yoakim, Christiane
, p. 7512 - 7517 (2013/02/23)
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.
