Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure–activity relationships associated with 4-fluoro-6-azaindole derivatives leading to …

…, C D'Arienzo, Y Sun, J Malinowski, Q Gao…

Index: Regueiro-Ren, Alicia; Xue, Qiufen M.; Swidorski, Jacob J.; Gong, Yi-Fei; Mathew, Marina; Parker, Dawn D.; Yang, Zheng; Eggers, Betsy; D'Arienzo, Celia; Sun, Yongnian; Malinowski, Jacek; Gao, Qi; Wu, Dedong; Langley, David R.; Colonno, Richard J.; Chien, Caly; Grasela, Dennis M.; Zheng, Ming; Lin, Pin-Fang; Meanwell, Nicholas A.; Kadow, John F. Journal of Medicinal Chemistry, 2013 , vol. 56, # 4 p. 1656 - 1669

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Citation Number: 27

Abstract

A series of highly potent HIV-1 attachment inhibitors with 4-fluoro-6-azaindole core heterocycles that target the viral envelope protein gp120 has been prepared. Substitution in the 7-position of the azaindole core with amides (12a, b), C-linked heterocycles (12c–l), and N-linked heterocycles (12m–u) provided compounds with subnanomolar potency in a pseudotype infectivity assay and good pharmacokinetic profiles in vivo. A predictive model ...