907200-66-2Relevant academic research and scientific papers
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle
He, Shanshan,Li, Kelin,Lin, Billy,Hu, Zongyi,Xiao, Jingbo,Hu, Xin,Wang, Amy Q.,Xu, Xin,Ferrer, Marc,Southall, Noel,Zheng, Wei,Aubé, Jeffrey,Schoenen, Frank J.,Marugan, Juan J.,Liang, T. Jake,Frankowski, Kevin J.
supporting information, p. 6364 - 6383 (2017/08/02)
Reliance on hepatitis C virus (HCV) replicon systems and protein-based screening assays has led to treatments that target HCV viral replication proteins. The model does not encompass other viral replication cycle steps such as entry, processing, assembly and secretion, or viral host factors. We previously applied a phenotypic high-throughput screening platform based on an infectious HCV system and discovered an aryloxazole-based anti-HCV hit. Structure-activity relationship studies revealed several compounds exhibiting EC50 values below 100 nM. Lead compounds showed inhibition of the HCV pseudoparticle entry, suggesting a different mode of action from existing HCV drugs. Hit 7a and lead 7ii both showed synergistic effects in combination with existing HCV drugs. In vivo pharmacokinetics studies of 7ii showed high liver distribution and long half-life without obvious hepatotoxicity. The lead compounds are promising as preclinical candidates for the treatment of HCV infection and as molecular probes to study HCV pathogenesis.
SUBSTITUTED ARYLOXAZOLES AND THEIR USE
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Page/Page column 56; 59, (2011/06/23)
The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
