HCV Polymerase Inhibitors
نویسندگان
چکیده
منابع مشابه
Non-nucleoside inhibitors of the HCV polymerase.
Chronic hepatitis C virus (HCV) infection is the leading cause of chronic liver disease. Current therapy using pegylated interferon-alpha with ribavirin is poorly tolerated and confers an overall sustained virological response around 56%. Compounds exhibiting an improved safety profile with similar or enhanced antiviral properties may represent future treatment options. Several drug discovery p...
متن کاملClassification of HCV NS5B Polymerase Inhibitors Using Support Vector Machine
Using a support vector machine (SVM), three classification models were built to predict whether a compound is an active or weakly active inhibitor based on a dataset of 386 hepatitis C virus (HCV) NS5B polymerase NNIs (non-nucleoside analogue inhibitors) fitting into the pocket of the NNI III binding site. For each molecule, global descriptors, 2D and 3D property autocorrelation descriptors wer...
متن کاملNatural Polymorphisms Conferring Resistance to HCV Protease and Polymerase Inhibitors in Treatment-Naïve HIV/HCV Co-Infected Patients in China
BACKGROUND The advent of direct-acting agents (DAAs) has improved treatment of HCV in HIV co-infection, but may be limited by primary drug resistance. This study reports the prevalence of natural polymorphisms conferring resistance to NS3/4A protease inhibitors and NS5B polymerase inhibitors in treatment-naïve HIV/HCV co-infected individuals in China. METHODS Population based NS3/4A sequencin...
متن کاملSynergy of a hepatitis C virus (HCV) NS4A antagonist in combination with HCV protease and polymerase inhibitors.
Rapid emergence of resistance to monotherapy with virus-specific inhibitors necessitates combination therapy. ACH-806 is a hepatitis C virus NS4A inhibitor with a novel mechanism of action and resistance pathway. This compound was synergistic with NS3 protease inhibitors and NS5B nucleoside and nonnucleoside polymerase inhibitors.
متن کاملDiscovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.
A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a-c and 12a-c from a weak-binding fragment-like s...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2013
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml400428b