Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase

Bioorganic & Medicinal Chemistry Letters
Frank RuebsamLeo Kirkovsky

Abstract

Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Among these, compound 4c displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b) <10 nM; EC(50) (1b)=34 nM) as well as good stability towards human liver microsomes (HLM t(1/2) =59 min).

References

Aug 19, 1999·The New England Journal of Medicine·M J AlterH S Margolis
May 31, 2002·Journal of Medicinal Chemistry·Daniel F VeberKenneth D Kopple
Dec 8, 2006·The New England Journal of Medicine·Jay H Hoofnagle, Leonard B Seeff
Jul 14, 2007·Current Topics in Medicinal Chemistry·Uwe Koch, Frank Narjes
Dec 11, 2007·Bioorganic & Medicinal Chemistry Letters·Todd D BosseAkhter Molla
May 20, 2008·Bioorganic & Medicinal Chemistry Letters·Frank RuebsamLeo Kirkovsky

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Citations

Jun 27, 2009·Pharmacology & Therapeutics·Claire GondeauPatrick Maurel
Jan 28, 2014·Journal of Chemical Information and Modeling·Patrisha Joseph ThereseNeerja Kaushik-Basu

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