Talamas, Francisco X.; Abbot, Sarah C.; Anand, Shalini; Brameld, Ken A.; Carter, David S.; Chen, Jun; Davis, Dana; de Vicente, Javier; Fung, Amy D.; Gong, Leyi; Harris, Seth F.; Inbar, Petra; Labadie, Sharada S.; Lee, Eun K.; Lemoine, Remy; Le Pogam, Sophie; Leveque, Vincent; Li, Jim; McIntosh, Joel; Najera, Isabel; Park, Jaehyeon; Railkar, Aruna; Rajyaguru, Sonal; Sangi, Michael; Schoenfeld, Ryan C.; Staben, Leanna R.; Tan, Yunchou; Taygerly, Joshua P.; Villasenor, Armando G.; Weller, Paul E. published the artcile< Discovery of N [4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]-methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase>, Application In Synthesis of 112253-70-0, the main research area is oxopyridinyl butylquinolinylphenyl methanesulfonamide preparation hepatitis C virus polymerase inhibitor.
In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we discuss our efforts that led to the identification of a bicyclic template with potent activity against the NS5B polymerase, a critical enzyme on the life cycle of HCV. In continuation of our exploration to improve the stilbene series, the 3,5,6,8-tetrasubstituted quinoline core was identified as replacement of the stilbene moiety. 6-Methoxy-2-(1H)-pyridone was identified among several heterocyclic headgroups to have the best potency. Solubility of the template was improved by replacing a planar aryl linker with a saturated pyrrolidine. Profiling of the most promising compounds led to the identification of quinoline I (RG7109), which was selected for advancement to clin. development.
Journal of Medicinal Chemistry published new progress about Antiviral agents (hepatitis C). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Application In Synthesis of 112253-70-0.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics