Douglas S Johnson

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
    Douglas S Johnson
    Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 19:2865-9. 2009
  2. ncbi Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
    Douglas S Johnson
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Future Med Chem 2:949-64. 2010
  3. ncbi Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder
    Douglas S Johnson
    Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:2621-5. 2011
  4. ncbi Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain
    Kay Ahn
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Chem Biol 16:411-20. 2009
  5. ncbi Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain
    Kay Ahn
    Pfizer Worldwide Research and Development, Groton, Connecticut, USA
    J Pharmacol Exp Ther 338:114-24. 2011
  6. ncbi Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, USA
    Bioorg Med Chem Lett 22:2906-11. 2012
  7. ncbi The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH)
    Marc B Skaddan
    Pfizer Worldwide Research and Development, Pfizer Inc, Eastern Point Road, Mail Stop 8274 1342, Groton, CT 06340, USA
    Nucl Med Biol 39:1058-67. 2012
  8. ncbi Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity
    Kyunghye Ahn
    Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Biochemistry 46:13019-30. 2007
  9. ncbi Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses
    Yasong Lu
    MS 220 4546, Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    J Pharmacol Exp Ther 342:366-75. 2012
  10. ncbi Novel γ-secretase modulators: a review of patents from 2008 to 2010
    Martin Pettersson
    Pfizer Worldwide Research and Development, Neuroscience Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA
    Expert Opin Ther Pat 21:205-26. 2011

Collaborators

Detail Information

Publications11

  1. ncbi Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)
    Douglas S Johnson
    Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
    Bioorg Med Chem Lett 19:2865-9. 2009
    ..Several compounds showed in vivo activity in a rat complete Freund's adjuvant (CFA) model of inflammatory pain...
  2. ncbi Strategies for discovering and derisking covalent, irreversible enzyme inhibitors
    Douglas S Johnson
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Future Med Chem 2:949-64. 2010
    ..Emerging proteomic technologies offer a means to systematically discriminate safe (selective) versus deleterious (nonselective) covalent inhibitors and thus should inspire their future design and development...
  3. ncbi Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder
    Douglas S Johnson
    Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    Bioorg Med Chem Lett 21:2621-5. 2011
    ..This strategy led to identification of PF-00217830 (2) with robust inhibition of sLMA (MED=0.3mg/kg) and DOI-induced head twitches in rats (31% and 78% at 0.3 and 1mg/kg) with no catalepsy observed at the highest dose tested (10 mg/kg)...
  4. ncbi Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain
    Kay Ahn
    Pfizer Global Research and Development, Groton, CT 06340, USA
    Chem Biol 16:411-20. 2009
    ..These data thus designate PF-3845 as a valuable pharmacological tool for in vivo characterization of the endocannabinoid system...
  5. ncbi Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain
    Kay Ahn
    Pfizer Worldwide Research and Development, Groton, Connecticut, USA
    J Pharmacol Exp Ther 338:114-24. 2011
    ..Based on its exceptional selectivity and in vivo efficacy, combined with long duration of action and optimal pharmacokinetic properties, PF-04457845 is a clinical candidate for the treatment of pain and other nervous system disorders...
  6. ncbi Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
    Martin Pettersson
    Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340, USA
    Bioorg Med Chem Lett 22:2906-11. 2012
    ..Lead compounds such as 35 and 43 have moderate to good in vitro potency and excellent selectivity against Notch. Good oral bioavailability was achieved as well as robust brain Aβ42 lowering activity at 100 mg/kg po dose...
  7. ncbi The synthesis and in vivo evaluation of [18F]PF-9811: a novel PET ligand for imaging brain fatty acid amide hydrolase (FAAH)
    Marc B Skaddan
    Pfizer Worldwide Research and Development, Pfizer Inc, Eastern Point Road, Mail Stop 8274 1342, Groton, CT 06340, USA
    Nucl Med Biol 39:1058-67. 2012
    ..We report here the synthesis and in vivo evaluation of [(18)F]PF-9811, a novel PET ligand for non-invasive imaging of FAAH in the brain...
  8. ncbi Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity
    Kyunghye Ahn
    Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
    Biochemistry 46:13019-30. 2007
    ....
  9. ncbi Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses
    Yasong Lu
    MS 220 4546, Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA
    J Pharmacol Exp Ther 342:366-75. 2012
    ..We further discuss the implications of our findings to drug discovery and development with regard to preclinical PK/PD characterization and clinical prediction of Aβ lowering in the brain...
  10. ncbi Novel γ-secretase modulators: a review of patents from 2008 to 2010
    Martin Pettersson
    Pfizer Worldwide Research and Development, Neuroscience Medicinal Chemistry, Eastern Point Road, Groton, CT 06340, USA
    Expert Opin Ther Pat 21:205-26. 2011
    ..It will be important to gain a better understanding of the specific target(s) that these GSMs interact with in order to facilitate future drug design efforts...
  11. ncbi Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist
    Snahel D Patel
    Pfizer Global Research and Development, Cambridge Laboratories, Cambridge, MA 02139, USA
    Bioorg Med Chem Lett 18:5689-93. 2008
    ..Structure-activity studies demonstrate the structural requirements for binding affinity, functional activity, and selectivity over other alpha(2)-AR subtypes...