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Current Enzyme Inhibition

Editor-in-Chief

ISSN (Print): 1573-4080
ISSN (Online): 1875-6662

Research Article

Synthesis and In Vitro Activity of Pyrrolo[3,4-d]pyrimidine-2,5-diones as Potential Non-nucleoside HCV Inhibitors

Author(s): Amany S. Mostafa, Serry A. El Bialy, Waleed A. Bayoumi, Youki Ueda, Masanori Ikeda, Nobuyuki Kato and Ali M. Abdelal

Volume 12, Issue 2, 2016

Page: [170 - 176] Pages: 7

DOI: 10.2174/1573408011666151013204142

Price: $65

Abstract

A new series of 1-methyl-4-phenyl-6-substituted-3,4,6,7-tetrahydro-1H-pyrrolo[3,4- d]pyrimidine-2,5-diones (9a-h) were investigated as potential non-nucleoside anti-HCV, through Renilla luciferase (RL) assay using HuH-7-derived OR6 assay system. The target derivatives 9a-h were synthesized in moderate to good yields through nucleophilic substitution, followed by subsequent cyclocondensation of the 6-bromomethyl dihydropyrimidine derivative 8 with the appropriate primary amine. Biological screening revealed that compound 9a (EC50 of 28 M) showed moderate anti-HCV activity; while compounds 9c, 9e and 9h showed weak activity.

Keywords: HCV inhibitors, HuH-7-derived OR6 assay, pyrrolo[3, 4-d]pyrimidine, Renilla Luciferase (RL) assay.

Graphical Abstract


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