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

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.

SUBMITTER: Ekkati AR

PROVIDER: S-EPMC3278212 | biostudies-literature | 2012 Feb

REPOSITORIES: biostudies-literature

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

Ekkati Anil R AR Bollini Mariela M Domaoal Robert A RA Spasov Krasimir A KA Anderson Karen S KS Jorgensen William L WL

Bioorganic & medicinal chemistry letters 20120105 4

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. ...[more]

PMID: 22269110

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