Research Topics
Species | Anthony B PinkertonSummaryAffiliation: Kalypsys Inc Country: USA Publications
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Publications
Diaryl substituted pyrazoles as potent CCR2 receptor antagonistsAnthony 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)...- Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitorsAnthony 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... - Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiatorsAnthony 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... - Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiatorsAnthony 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... - 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)... - Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenonesAnthony 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)... - Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptorEssa 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... - Phenyl-tetrazolyl acetophenones: discovery of positive allosteric potentiatiors for the metabotropic glutamate 2 receptorAnthony 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...