Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors

  • Bioorg Med Chem Lett. 2003 Mar 24;13(6):1215-9. doi: 10.1016/s0960-894x(03)00059-3.
Xuechun Zhang  1 ,  Godwin C G Pais ,  Evguenia S Svarovskaia ,  Christophe Marchand ,  Allison A Johnson ,  Rajeshri G Karki ,  Marc C Nicklaus ,  Vinay K Pathak ,  Yves Pommier ,  Terrence R Burke
Affiliations
  • 1. Laboratory of Medicinal Chemistry, Center for Cancer Research, National Cancer Institute, National Institutes of Health, MD, USA.
PMID: 12643946 DOI: 10.1016/s0960-894x(03)00059-3
Abstract

Aryl beta-diketo acids (ADK) comprise a general class of potent HIV-1 integrase (IN) inhibitors, which can exhibit selective inhibition of strand transfer reactions in extracellular recombinant IN assays and provide potent Antiviral effects in HIV-infected cells. Recent studies have shown that polycyclic aryl or aryl rings bearing aryl-containing substituents are components of potent members of this class. Reported herein is the first use of azido functionality as an aryl replacement in beta-diketo acid IN inhibitors. The ability of azido-containing inhibitors to exhibit potent inhibition of IN and Antiviral protection in HIV-infected cells, renders the azide group of potential value in the further development of ADK-based IN inhibitors.