EMAIL THIS PAGE TO A FRIEND

Bioorganic & medicinal chemistry letters

Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase.


PMID 22542020

Abstract

Aryl dihydrouracil derivatives were identified from high throughput screening as potent inhibitors of HCV NS5B polymerase. The aryl dihydrouracil derivatives were shown to be non-competitive with respect to template RNA and elongation nucleotide substrates. They demonstrated genotype 1 specific activity towards HCV NS5B polymerases. Structure activity relationships and genotype specific activities of aryl dihydrouracil derivatives suggested that they bind to the palm initiation nucleotide pocket, a hypothesis which was confirmed by studies with polymerases containing mutations in various inhibitor binding sites. Therefore, aryl dihydrouracil derivatives represent a novel class of palm initiation site inhibitors of HCV NS5B polymerase.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

D7628
Dihydrouracil
C4H6N2O2