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.

Polymerases:

Topics:

Modulators/Inhibitors, Health/Disease, RNase H Activity

Status:

new topics/pols set partial results complete validated

Results:

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