HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent

  • J Med Chem. 2006 Jan 26;49(2):445-7. doi: 10.1021/jm0508890.
Vasu Nair  1 ,  Guochen Chi ,  Roger Ptak ,  Nouri Neamati
Affiliations
  • 1. The Center for Drug Discovery, Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602, USA. [email protected]
PMID: 16420027 DOI: 10.1021/jm0508890
Abstract

HIV Integrase is essential for HIV replication. However, there are currently no integrase inhibitors in clinical use for AIDS. We have discovered a conceptually new beta-diketo acid that is a powerful inhibitor of both the 3'-processing and strand transfer steps of HIV-1 integrase. The in vitro anti-HIV data of this inhibitor were remarkable as exemplified by its highly potent Antiviral therapeutic efficacy against HIV(TEKI) and HIV-1(NL4)(-)(3) replication in PBMC (TI >4,000 and >10,000, respectively).