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. pmc HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter
    Alice Kiselyuk
    Department of Bioengineering, University of California, San Diego, La Jolla, CA 92093, USA
    Chem Biol 19:806-18. 2012
  8. 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
  9. 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

Collaborators

Detail Information

Publications9

  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. pmc HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter
    Alice Kiselyuk
    Department of Bioengineering, University of California, San Diego, La Jolla, CA 92093, USA
    Chem Biol 19:806-18. 2012
    ..The discovery of bioactive modulators for HNF4α raises the possibility that diseases involving HNF4α, such as diabetes and cancer, might be amenable to pharmacologic intervention by modulation of HNF4α activity...
  8. 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...
  9. 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...