Title: Pyridobenzothiazole derivatives as new chemotype targeting the HCV NS5B polymerase
Authors: Manfroni, Giuseppe ×
Meschini, Francesco
Barreca, Maria Letizia
Leyssen, Pieter
Samuele, Alberta
Iraci, Nunzio
Sabatini, Stefano
Massari, Serena
Maga, Giovanni
Neyts, Johan
Cecchetti, Violetta #
Issue Date: Jan-2012
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:20 issue:2 pages:866-76
Abstract: Hepatitis C virus (HCV) infection has been recognized as the major cause of liver failure that can lead to hepatocellular carcinoma. Among all the HCV proteins, NS5B polymerase represents a leading target for drug discovery strategies. Herein, we describe our initial research efforts towards the identification of new chemotypes as allosteric NS5B inhibitors. In particular, the design, synthesis, in vitro anti-NS5B and in cellulo anti-HCV evaluation of a series of 1-oxo-1H-pyrido[2,1-b][1,3]benzothiazole-4-carboxylate derivatives are reported. Some of the newly synthesized compounds showed an IC(50) ranging from 11 to 23 μM, and molecular modeling and biochemical studies suggested that the thumb domain could be the target site for this new class of NS5B inhibitors.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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