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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ekkati AR,Bollini M,Domaoal RA,Spasov KA,Anderson KS,Jorgensen WL

doi

10.1016/j.bmcl.2011.12.132

subject

Has Abstract

pub_date

2012-02-15 00:00:00

pages

1565-8

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01814-2

journal_volume

22

pub_type

杂志文章

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