Literature DB >> 17269759

Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate.

Martin J Slater1, Elizabeth M Amphlett, David M Andrews, Gianpaolo Bravi, George Burton, Anne G Cheasty, John A Corfield, Malcolm R Ellis, Rebecca H Fenwick, Stephanie Fernandes, Rossella Guidetti, David Haigh, C David Hartley, Peter D Howes, Deborah L Jackson, Richard L Jarvest, Victoria L H Lovegrove, Katrina J Medhurst, Nigel R Parry, Helen Price, Pritom Shah, Onkar M P Singh, Richard Stocker, Pia Thommes, Claire Wilkinson, Alan Wonacott.   

Abstract

Optimization of a pyrrolidine-based template using structure-based design and physicochemical considerations has provided a development candidate 20b (3082) with submicromolar potency in the HCV replicon and good pharmacokinetic properties.

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Year:  2007        PMID： 17269759     DOI： 10.1021/jm061207r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  9 in total

1.  Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry.

Authors:  Marco Potowski; Verena B K Kunig; Florian Losch; Andreas Brunschweiger
Journal:  Medchemcomm       Date:  2019-02-26       Impact factor: 3.597

2.  Stereoselective Synthesis of Quaternary Proline Analogues.

Authors:  M Isabel Calaza; Carlos Cativiela
Journal:  European J Org Chem       Date:  2008

3.  QSAR study of C allosteric binding site of HCV NS5B polymerase inhibitors by support vector machine.

Authors:  Eslam Pourbasheer; Siavash Riahi; Mohammad Reza Ganjali; Parviz Norouzi
Journal:  Mol Divers       Date:  2010-10-08       Impact factor: 2.943

4.  Chiral gold(I) vs chiral silver complexes as catalysts for the enantioselective synthesis of the second generation GSK-hepatitis C virus inhibitor.

Authors:  María Martín-Rodríguez; Carmen Nájera; José M Sansano; Abel de Cózar; Fernando P Cossío
Journal:  Beilstein J Org Chem       Date:  2011-07-19       Impact factor: 2.883

5.  Antiviral therapy for hepatitis C virus: beyond the standard of care.

Authors:  Leen Delang; Lotte Coelmont; Johan Neyts
Journal:  Viruses       Date:  2010-03-29       Impact factor: 5.818

6.  Design and synthesis of L- and D-phenylalanine derived rhodanines with novel C5-arylidenes as inhibitors of HCV NS5B polymerase.

Authors:  Bhargav A Patel; Ramalingam Krishnan; Nikhil Khadtare; K R Gurukumar; Amartya Basu; Payal Arora; Aaditya Bhatt; Maulik R Patel; Dibyendu Dana; Sanjai Kumar; Neerja Kaushik-Basu; Tanaji T Talele
Journal:  Bioorg Med Chem       Date:  2013-03-31       Impact factor: 3.641

7.  MAP-kinase regulated cytosolic phospholipase A2 activity is essential for production of infectious hepatitis C virus particles.

Authors:  Nicolas Menzel; Wolfgang Fischl; Kathrin Hueging; Dorothea Bankwitz; Anne Frentzen; Sibylle Haid; Juliane Gentzsch; Lars Kaderali; Ralf Bartenschlager; Thomas Pietschmann
Journal:  PLoS Pathog       Date:  2012-07-26       Impact factor: 6.823

8.  Multiple virtual screening approaches for finding new hepatitis C virus RNA-dependent RNA polymerase inhibitors: structure-based screens and molecular dynamics for the pursue of new poly pharmacological inhibitors.

Authors:  Mahmoud Elhefnawi; Mohammad ElGamacy; Mohamed Fares
Journal:  BMC Bioinformatics       Date:  2012-12-13       Impact factor: 3.169

9.  Insight into ligand selectivity in HCV NS5B polymerase: molecular dynamics simulations, free energy decomposition and docking.

Authors:  Tong Li; Matheus Froeyen; Piet Herdewijn
Journal:  J Mol Model       Date:  2009-05-26       Impact factor: 1.810
  9 in total

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