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Your search keyword '"Ravi, Rajagopalan"' showing total 3 results
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3 results on '"Ravi, Rajagopalan"'

1. Quinolones as HCV NS5B polymerase inhibitors

Author

Huiyong Hu, Tony Ton, Dange Vijay Kumar, Roopa Rai, Michael J. Green, Isabelle Lehoux, Ravi Rajagopalan, Ken A. Brameld, John R. Somoza, Michael B. Shaghafi, James W. Janc, Nhat To, Yu M. Xia, and Wendy B. Young

Subjects
viruses, Hepatitis C virus, Hepacivirus, Clinical Biochemistry, Allosteric regulation, Pharmaceutical Science, Quinolones, Viral Nonstructural Proteins, medicine.disease_cause, Crystallography, X-Ray, Biochemistry, Antiviral Agents, Virus, chemistry.chemical_compound, Structure-Activity Relationship, Allosteric Regulation, Drug Discovery, medicine, Computer Simulation, Enzyme Inhibitors, Molecular Biology, NS5B, Binding Sites, biology, Ribavirin, Organic Chemistry, virus diseases, Quinoline analog, biology.organism_classification, Small molecule, Virology, digestive system diseases, chemistry, Molecular Medicine
Abstract

Hepatitis C virus (HCV) infection is treated with a combination of peginterferon alfa-2a/b and ribavirin. To address the limitations of this therapy, numerous small molecule agents are in development, which act by directly affecting key steps in the viral life-cycle. Herein we describe our discovery of quinolone derivatives, novel small-molecules that inhibit NS5b polymerase, a key enzyme of the viral life-cycle. A crystal structure of a quinoline analog bound to NS5B reveals that this class of compounds binds to allosteric site-II (non-nucleoside inhibitor-site 2, NNI-2) of this protein.

Published
2010

2. HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives

Author

Shawn Misialek, Lisa Hooi, Guangyi Wang, Yanzhen He, Antitsa Dimitrova Stoycheva, Debasis Das, Mougang Hu, Jun Sun, Donald Ruhrmund, Leonid Beigelman, Scott D. Seiwert, Karl Kossen, Brad O. Buckman, Jianhua Huang, and P. T. Ravi Rajagopalan

Subjects
Magnetic Resonance Spectroscopy, Stereochemistry, viruses, Hepatitis C virus, Chemistry, Pharmaceutical, Clinical Biochemistry, Pharmaceutical Science, Hepacivirus, Naphthols, In Vitro Techniques, Naphthalenes, Viral Nonstructural Proteins, medicine.disease_cause, Benzothiadiazines, Biochemistry, Chemical synthesis, Antiviral Agents, chemistry.chemical_compound, Inhibitory Concentration 50, Structure-Activity Relationship, Drug Discovery, medicine, Animals, Humans, Replicon, Enzyme Inhibitors, Molecular Biology, chemistry.chemical_classification, Bicyclic molecule, biology, Molecular Structure, Organic Chemistry, virus diseases, biochemical phenomena, metabolism, and nutrition, Hepatitis C, digestive system diseases, In vitro, Enzyme, chemistry, Models, Chemical, Benzothiadiazine, Enzyme inhibitor, Drug Design, biology.protein, Molecular Medicine
Abstract

2-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition and replicon activity are discussed.

Published
2009

3. HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives

Author

Shawn Misialek, P. T. Ravi Rajagopalan, Karl Kossen, Guangyi Wang, Xiaomin Wu, Laiguo Zhang, Debasis Das, Lisa Hooi, Donald Ruhrmund, Scott D. Seiwert, Brad O. Buckman, and Leonid Beigelman

Subjects
Magnetic Resonance Spectroscopy, Stereochemistry, viruses, Chemistry, Pharmaceutical, Clinical Biochemistry, Pharmaceutical Science, Hepacivirus, In Vitro Techniques, Viral Nonstructural Proteins, Benzothiadiazines, Biochemistry, Antiviral Agents, Ns5b polymerase, Inhibitory Concentration 50, Structure-Activity Relationship, Drug Discovery, Animals, Replicon, Enzyme Inhibitors, Molecular Biology, Molecular Structure, Chemistry, Organic Chemistry, virus diseases, biochemical phenomena, metabolism, and nutrition, Hepatitis C, digestive system diseases, In vitro, Models, Chemical, Drug Design, Molecular Medicine, Quinolizines
Abstract

3-(1,1-Dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives as potential anti-HCV drugs targeting NS5B polymerase have been investigated. Their synthesis, HCV NS5B polymerase inhibition, and replicon activity are discussed.

Published
2009

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