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Bioorg Med Chem Lett. 2012 Feb 15;22(4):1565-8. doi: 10.1016/j.bmcl.2011.12.132. Epub 2012 Jan 5.

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

Author information

1
Department of Chemistry, Yale University, New Haven, CT 06520, USA.

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.

PMID:
22269110
PMCID:
PMC3278212
DOI:
10.1016/j.bmcl.2011.12.132
[Indexed for MEDLINE]
Free PMC Article

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