title: Biologically-validated HIV integrase inhibitors with nucleobase scaffolds: structure, synthesis, chemical biology, molecular modeling, and antiviral activity.
abstract: Integrase, an enzyme of the pol gene of HIV, is a significant viral target for the discovery of anti-HIV agents. In this presentation, we report on the continuation of our work on the discovery of diketo acids, constructed on nucleobase scaffolds, that are inhibitors of HIV integrase. An example of our synthetic approach to inhibitors with purine nucleobase scaffolds is given. Comparison is made between integrase inhibition data arising from compounds with pyrimidine versus purine nucleobase scaffold. Antiviral results are cited.
authors: Center for Drug Discovery and the Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602-2352, USA. vnair@rx.uga.edu
authors: Vasu
authors: V
authors: Nair
authors: Vinod
authors: V
authors: Uchil
authors: Guochen
authors: G
authors: Chi
authors: Iwona
authors: I
authors: Dams
authors: Arthur
authors: A
authors: Cox
authors: Byung
authors: B
authors: Seo
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D009705:Nucleosides / Q000737:chemistry*; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D000998:Antiviral Agents; D019428:HIV Integrase Inhibitors; D009705:Nucleosides; D011687:Purines