Biologically-validated HIV integrase inhibitors with nucleobase scaffolds: structure, synthesis, chemical biology, molecular modeling, and antiviral activity.
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.
Nair
Vasu
V
Center for Drug Discovery and the Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602-2352, USA. vnair@rx.uga.edu
Uchil
Vinod
V
Chi
Guochen
G
Dams
Iwona
I
Cox
Arthur
A
Seo
Byung
B
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
D000998:Antiviral Agents; D019428:HIV Integrase Inhibitors; D009705:Nucleosides; D011687:Purines