Imidazo[1,2-a]pyridines That Directly Interact with Hepatitis C NS4B: Initial Preclinical Characterization

التفاصيل البيبلوغرافية
العنوان: Imidazo[1,2-a]pyridines That Directly Interact with Hepatitis C NS4B: Initial Preclinical Characterization
المؤلفون: Subramanian Baskaran, Renae M. Crosby, John W. Seal, Zhiping Z. Xiong, Mi Xie, Hamilton D. Dickson, Roopa Rai, Pek Yoke Chong, Uli Schmitz, Jeffrey J. Pouliot, Derek J. Parks, J. Brad Shotwell, Amanda Mathis, Michael Thomson, Daniel J. Price, Jing Fang, Jack Maung, Katrina L. Creech, Dulce Garrido, Vincent W.-F. Tai, Andrew J. Peat
المصدر: ACS Medicinal Chemistry Letters. 3:565-569
بيانات النشر: American Chemical Society (ACS), 2012.
سنة النشر: 2012
مصطلحات موضوعية: business.industry, viruses, Hepatitis C virus, Organic Chemistry, virus diseases, Hepatitis C, Synergistic combination, Pharmacology, medicine.disease, medicine.disease_cause, Biochemistry, Small molecule, digestive system diseases, In vitro, Drug Discovery, medicine, Replicon, business, IC50, EC50
الوصف: A series of imidazo[1,2-a]pyridines which directly bind to HCV Non-Structural Protein 4B (NS4B) is described. This series demonstrates potent in vitro inhibition of HCV replication (EC50 < 10 nM), direct binding to purified NS4B protein (IC50 < 20 nM), and an HCV resistance pattern associated with NS4B (H94N/R, V105L/M, F98L) that are unique among reported HCV clinical assets, suggestive of the potential for additive or synergistic combination with other small molecule inhibitors of HCV replication.
تدمد: 1948-5875
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6d17cf185305bf4917b0cb0a406345b
https://doi.org/10.1021/ml300090x
حقوق: OPEN
رقم الأكسشن: edsair.doi.dedup.....f6d17cf185305bf4917b0cb0a406345b
قاعدة البيانات: OpenAIRE