title: Beta-diketo acids with purine nucleobase scaffolds: novel, selective inhibitors of the strand transfer step of HIV integrase.
abstract: The HIV pol gene encodes three viral enzymes that are required for its replication. While drug discovery involving the viral targets, reverse transcriptase and protease, has resulted in useful therapeutic agents, such efforts on HIV integrase have not produced a single FDA-approved drug. In the work focused on the discovery of inhibitors of HIV integrase, we have synthesized new beta-diketo acids with purine nucleobase scaffolds that are potent inhibitors of the strand transfer steps of wild-type HIV-1 integrase.
authors.affiliation: The Center for Drug Discovery and the Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA 30602, USA. vnair@rx.uga.edu
authors.forename: Vasu
authors.initials: V
authors.lastname: Nair
authors.forename: Vinod
authors.initials: V
authors.lastname: Uchil
authors.forename: Nouri
authors.initials: N
authors.lastname: Neamati
mesh_terms: D000143:Acids / Q000737:chemistry*; D019428:HIV Integrase Inhibitors / Q000737:chemistry*; D008958:Models, Molecular; D011687:Purines / Q000737:chemistry*
chemical_list: D000143:Acids; D019428:HIV Integrase Inhibitors; D011687:Purines