Synthesis and evaluation of novel HCV replication inhibitors.

Autor: McGowan DC; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium. dmcgowan@its.jnj.com., Khamlichi MD; Villapharma Research, Parque Tecnológico de Fuente Álamo, Ctra. El Estrecho-Lobosillo, Km. 2,5- Av. Azul, 30320, Fuente Álamo de Murcia, Murcia, Spain., De Groot A; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium., Pauwels F; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium., Delouvroy F; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium., Van Emelen K; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium., Simmen K; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium., Raboisson P; Janssen Infectious Diseases BVBA, Turnhoutseweg 30, 2340, Beerse, Belgium.
Jazyk: angličtina
Zdroj: Molecular diversity [Mol Divers] 2017 May; Vol. 21 (2), pp. 475-481. Date of Electronic Publication: 2017 Mar 14.
DOI: 10.1007/s11030-017-9733-z
Abstrakt: Direct acting antiviral agents to cure hepatitis C virus (HCV) infection has emerged as the gold standard therapy. Along with protease inhibitors, nucleoside polymerase inhibitors and non-nucleoside polymerase inhibitors, the inhibition of NS5a has proved to be an effective way to treat HCV patients. Here we report on novel HCV NS5a inhibitors which were synthesized and evaluated in the HCV replicon assay. A series of inhibitors were formed by a cycloaddition reaction in parallel to establish new leads and explore the effects of unsymmetrical cap substitution. This led to the identification of several triazoles with picomolar potency in vitro against hepatitis C virus.
Databáze: MEDLINE
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