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Small molecule inhibitors of HIV RT Ribonuclease H.

Abstract：

:Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established and time of addition studies were consistent with inhibition of RT-mediated HIV replication.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Di Grandi M,Olson M,Prashad AS,Bebernitz G,Luckay A,Mullen S,Hu Y,Krishnamurthy G,Pitts K,O'Connell J

doi

10.1016/j.bmcl.2009.10.043

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

398-402

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01444-9

journal_volume

20

pub_type

杂志文章

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