Anthony B Pinkerton

Summary

Affiliation: Kalypsys Inc
Country: USA

Publications

  1. ncbi request reprint Diaryl substituted pyrazoles as potent CCR2 receptor antagonists
    Anthony B Pinkerton
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:807-13. 2007
  2. ncbi request reprint Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors
    Anthony B Pinkerton
    Department of Medicinal Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:3562-9. 2007
  3. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:1565-71. 2005
  4. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5867-72. 2004
  5. ncbi request reprint 3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
    Rowena V Cube
    Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:2389-93. 2005
  6. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5329-32. 2004
  7. ncbi request reprint Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptor
    Essa Hu
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5071-4. 2004
  8. ncbi request reprint Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor
    Anthony B Pinkerton
    Merck Research Laboratories San Diego, 3535 General Atomics Court, San Diego, California 92121, USA
    J Med Chem 47:4595-9. 2004

Detail Information

Publications8

  1. ncbi request reprint Diaryl substituted pyrazoles as potent CCR2 receptor antagonists
    Anthony B Pinkerton
    Department of Medicinal Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:807-13. 2007
    ..Structure-activity relationship studies directed toward improving the potency led to the discovery of 23 (IC50 = 6 nM)...
  2. ncbi request reprint Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors
    Anthony B Pinkerton
    Department of Medicinal Chemistry, Kalypsys, Inc, 10420 Wateridge Circle, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 17:3562-9. 2007
    ..SAR studies led to the synthesis of 33, which was co-crystallized with KSP and determined to bind to an allosteric pocket previously described for other known KSP inhibitors...
  3. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:1565-71. 2005
    ..Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50=186 nM), which displayed activity in a rodent model for schizophrenia...
  4. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5867-72. 2004
    ..Structure-activity relationship studies directed toward replacement of the tetrazole in the initial lead led to the discovery of 16 (EC(50)=340 nM), which showed improved brain penetration over the initial lead...
  5. ncbi request reprint 3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
    Rowena V Cube
    Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:2389-93. 2005
    ..p., brain level of 5700 nM)...
  6. ncbi request reprint Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones
    Anthony B Pinkerton
    Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5329-32. 2004
    ..Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC(50)=93nM, 128% potentiation)...
  7. ncbi request reprint Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptor
    Essa Hu
    Department of Medicinal Chemistry, Merck Research Laboratories, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:5071-4. 2004
    ..Pyrimidine methyl anilines as potent and selective mGlu2 potentiators are described. Findings from the structure-activity-relationship investigations are discussed...
  8. ncbi request reprint Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptor
    Anthony B Pinkerton
    Merck Research Laboratories San Diego, 3535 General Atomics Court, San Diego, California 92121, USA
    J Med Chem 47:4595-9. 2004
    ..This represents the first example of the efficacy of mGlu2 receptor potentiators in these models...