Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase

  • Bioorg Med Chem Lett. 2012 Feb 15;22(4):1565-8. doi: 10.1016/j.bmcl.2011.12.132.
Anil R Ekkati  1 ,  Mariela Bollini ,  Robert A Domaoal ,  Krasimir A Spasov ,  Karen S Anderson ,  William L Jorgensen
Affiliations
  • 1. Department of Chemistry, Yale University, New Haven, CT 06520, USA.
PMID: 22269110 DOI: 10.1016/j.bmcl.2011.12.132
Abstract

Design of non-nucleoside inhibitors of HIV-1 Reverse Transcriptase is being pursued with computational guidance. Extension of azine-containing inhibitors into the entrance channel between Lys103 and Glu138 has led to the discovery of potent and structurally novel derivatives including dimeric inhibitors in an NNRTI-linker-NNRTI motif.