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

Bioorganic & Medicinal Chemistry Letters
2012.0

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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