Novel hepatitis C virus replicon inhibitors: synthesis and structure-activity relationships of fused pyrimidine derivatives

A Chris Krueger; Darold L Madigan; David W Beno; David A Betebenner; Robert Carrick; Brian E Green; Wenping He; Dachun Liu; Clarence J Maring; Keith F McDaniel; Hongmei Mo; Akhteruzzaman Molla; Christopher E Motter; Tami J Pilot-Matias; Michael D Tufano; Dale J Kempf

doi:10.1016/j.bmcl.2012.01.096

Novel hepatitis C virus replicon inhibitors: synthesis and structure-activity relationships of fused pyrimidine derivatives

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2212-5. doi: 10.1016/j.bmcl.2012.01.096. Epub 2012 Feb 2.

Authors

A Chris Krueger¹, Darold L Madigan, David W Beno, David A Betebenner, Robert Carrick, Brian E Green, Wenping He, Dachun Liu, Clarence J Maring, Keith F McDaniel, Hongmei Mo, Akhteruzzaman Molla, Christopher E Motter, Tami J Pilot-Matias, Michael D Tufano, Dale J Kempf

Affiliation

¹ Abbott Labs, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA. [email protected]

PMID: 22342631
DOI: 10.1016/j.bmcl.2012.01.096

Abstract

The synthesis of several pyrido[2,3-d]pyrimidine and pyrimido[4,5-d]pyrimidine analogs is described with one such analog possessing subnanomolar potency in both genotype 1a and 1b cell culture HCV replicon assays.

MeSH terms

Antiviral Agents / chemical synthesis*
Antiviral Agents / pharmacology
Cell Line, Tumor
Genotype
Hepacivirus / drug effects*
Hepacivirus / physiology
Humans
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology
RNA, Viral / antagonists & inhibitors*
RNA, Viral / biosynthesis
Replicon / drug effects
Structure-Activity Relationship
Virus Replication / drug effects

Substances

Antiviral Agents
Pyrimidines
RNA, Viral