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- …

M Tremblay, P Bonneau, Y Bousquet, P DeRoy…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7512 - 7517

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被引用次数: 17

摘要

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.