2. Academic Validation
  3. Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase

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

Affiliation

  • 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.

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