Richard L Jarvest

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi request reprint Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK
    Bioorg Med Chem Lett 13:1265-8. 2003
  2. pmc Variable sensitivity to bacterial methionyl-tRNA synthetase inhibitors reveals subpopulations of Streptococcus pneumoniae with two distinct methionyl-tRNA synthetase genes
    Daniel R Gentry
    Department of Microbiology, Microbial, Musculoskeletal, and Proliferative Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Antimicrob Agents Chemother 47:1784-9. 2003
  3. ncbi request reprint Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 14:3937-41. 2004
  4. ncbi request reprint Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:2305-9. 2005
  5. ncbi request reprint Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate
    Martin J Slater
    Infectious Diseases CEDD and Medicinal Discovery Research, GlaxoSmithKline, GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom
    J Med Chem 50:897-900. 2007
  6. ncbi request reprint Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 13:665-8. 2003
  7. ncbi request reprint The antimicrobial natural product chuangxinmycin and some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase
    Murray J Brown
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 12:3171-4. 2002
  8. doi request reprint 6-Alkylquinolone-3-carboxylic acid tethered to macrolides synthesis and antimicrobial profile
    Samra Kapić
    GlaxoSmithKline Research Centre Zagreb Ltd, Prilaz baruna Filipovica 29, HR 10000 Zagreb, Croatia
    Bioorg Med Chem 18:6569-77. 2010
  9. ncbi request reprint Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens
    Richard L Jarvest
    J Med Chem 45:1959-62. 2002

Collaborators

Detail Information

Publications9

  1. ncbi request reprint Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK
    Bioorg Med Chem Lett 13:1265-8. 2003
    ..Combination of this linker with an optimal substituted aryl right-hand side has resulted in a compound with exceptionally good antibacterial activity against staphylococci and enterococci, including antibiotic resistant strains...
  2. pmc Variable sensitivity to bacterial methionyl-tRNA synthetase inhibitors reveals subpopulations of Streptococcus pneumoniae with two distinct methionyl-tRNA synthetase genes
    Daniel R Gentry
    Department of Microbiology, Microbial, Musculoskeletal, and Proliferative Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Antimicrob Agents Chemother 47:1784-9. 2003
    ..pneumoniae is the result of horizontal gene transfer which has been driven by selection for resistance to some unknown class of naturally occurring antibiotics with similarities to recently reported synthetic MetS inhibitors...
  3. ncbi request reprint Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 14:3937-41. 2004
    ..Compound 46 demonstrated very good antibacterial activity against panels of antibiotic-resistant staphylococci and enterococci...
  4. ncbi request reprint Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:2305-9. 2005
    ..Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition...
  5. ncbi request reprint Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate
    Martin J Slater
    Infectious Diseases CEDD and Medicinal Discovery Research, GlaxoSmithKline, GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom
    J Med Chem 50:897-900. 2007
    ..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...
  6. ncbi request reprint Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity
    Richard L Jarvest
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 13:665-8. 2003
    ..The best compounds showed excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics...
  7. ncbi request reprint The antimicrobial natural product chuangxinmycin and some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase
    Murray J Brown
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 12:3171-4. 2002
    ..The only analogue to show inhibition comparable to chuangxinmycin also had antibacterial activity. WRS inhibition may contribute to the antibacterial action of chuangxinmycin...
  8. doi request reprint 6-Alkylquinolone-3-carboxylic acid tethered to macrolides synthesis and antimicrobial profile
    Samra Kapić
    GlaxoSmithKline Research Centre Zagreb Ltd, Prilaz baruna Filipovica 29, HR 10000 Zagreb, Croatia
    Bioorg Med Chem 18:6569-77. 2010
    ....
  9. ncbi request reprint Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens
    Richard L Jarvest
    J Med Chem 45:1959-62. 2002
    ..Compound 11 demonstrated in vivo efficacy in an S. aureus rat abscess infection model...