Romuald Corbau

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. pmc Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1
    Romuald Corbau
    Department of Discovery Biology, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 54:4451-63. 2010
  2. doi Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:5857-60. 2009
  3. doi Pyrazole NNRTIs 3: optimisation of physicochemical properties
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT 13 9NJ, UK
    Bioorg Med Chem Lett 19:5603-6. 2009
  4. doi Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays
    Lyn H Jones
    Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Med Chem 52:1219-23. 2009
  5. doi HCV-NS3 inhibitors: determination of their kinetic parameters and mechanism
    Maria Victoria Flores
    Discovery Biology Department, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK
    Biochim Biophys Acta 1794:1441-8. 2009
  6. doi Pyrazole NNRTIs 1: design and initial optimisation of a novel template
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:5599-602. 2009

Detail Information

Publications6

  1. pmc Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1
    Romuald Corbau
    Department of Discovery Biology, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom
    Antimicrob Agents Chemother 54:4451-63. 2010
    ..Altogether lersivirine is a highly potent and selective NNRTI, with excellent efficacy against NNRTI-resistant viruses...
  2. doi Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:5857-60. 2009
    ..We describe our analysis and conclusions leading to the selection of alcohol 5 (UK-453,061, lersivirine) for clinical development...
  3. doi Pyrazole NNRTIs 3: optimisation of physicochemical properties
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT 13 9NJ, UK
    Bioorg Med Chem Lett 19:5603-6. 2009
    ..In contrast replacement of the substituted benzyl group with corresponding phenylthio or phenoxy groups resulted in marked improvements in potency, ligand efficiency (LE) and LLE...
  4. doi Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays
    Lyn H Jones
    Discovery Chemistry, Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom
    J Med Chem 52:1219-23. 2009
    ....
  5. doi HCV-NS3 inhibitors: determination of their kinetic parameters and mechanism
    Maria Victoria Flores
    Discovery Biology Department, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK
    Biochim Biophys Acta 1794:1441-8. 2009
    ..In the case of BILN-2061, a better fit is obtained using a one-step model, indicating that the loss of potency is due to an increase in the off-rate of the EI complex...
  6. doi Pyrazole NNRTIs 1: design and initial optimisation of a novel template
    Charles E Mowbray
    Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK
    Bioorg Med Chem Lett 19:5599-602. 2009
    ..These compounds are active against wild type reverse transcriptase (RT) and retain activity against clinically important mutants...