Shaun R Stauffer

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1788-92. 2007
  2. ncbi request reprint Small molecule inhibition of the Bcl-X(L)-BH3 protein-protein interaction: proof-of-concept of an in vivo chemopotentiator ABT-737
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 3 P O Box 4, West Point, PA 19486, USA
    Curr Top Med Chem 7:961-5. 2007
  3. doi request reprint Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 51:6259-62. 2008
  4. ncbi request reprint Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites
    Georgia B McGaughey
    Department of Molecular Systems, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1117-21. 2007
  5. ncbi request reprint Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA
    J Med Chem 46:5294-7. 2003
  6. doi request reprint Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronates
    James Z Deng
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
    Org Lett 11:345-7. 2009
  7. pmc T-type calcium channels regulate cortical plasticity in-vivo. [corrected]
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, Philadelphia, Pennsylvania, USA
    Neuroreport 20:257-62. 2009
  8. ncbi request reprint Fluorescence resonance energy transfer (FRET) as a high-throughput assay for coupling reactions. Arylation of amines as a case study
    Shaun R Stauffer
    Department of Chemistry, Yale University, P O Box 208107, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 125:6977-85. 2003
  9. ncbi request reprint Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid
    Matthew G Stanton
    J Med Chem 50:3431-3. 2007

Collaborators

Detail Information

Publications9

  1. ncbi request reprint Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1788-92. 2007
    ....
  2. ncbi request reprint Small molecule inhibition of the Bcl-X(L)-BH3 protein-protein interaction: proof-of-concept of an in vivo chemopotentiator ABT-737
    Shaun R Stauffer
    Department of Medicinal Chemistry, Merck Research Laboratories, WP14 3 P O Box 4, West Point, PA 19486, USA
    Curr Top Med Chem 7:961-5. 2007
    ..This review will focus on the recent advances surrounding the non-peptidic Bcl-2/X(L) inhibitor ABT-737 developed by Abbot laboratories and highlight the key structural characteristics found within this unique BH3 alpha-helical mimetic...
  3. doi request reprint Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    J Med Chem 51:6259-62. 2008
    ..Using the crystal structure as a guide, potent compounds with good brain penetration were designed...
  4. ncbi request reprint Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites
    Georgia B McGaughey
    Department of Molecular Systems, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:1117-21. 2007
    ..These X-ray structures were used to correlate K(i) values, which span over five orders of magnitude, with the calculated interaction energy, using the Merck Molecular Force Field for a series of 19 tertiary carbinamine inhibitors...
  5. ncbi request reprint Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics
    James C Barrow
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, Pennsylvania 19486, USA
    J Med Chem 46:5294-7. 2003
    ..Further, 10j accelerated clot lysis in vitro and was shown to be efficacious in a primate model of thrombosis...
  6. doi request reprint Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronates
    James Z Deng
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
    Org Lett 11:345-7. 2009
    ..Use of this methodology affords greatly enhanced yields of these notoriously difficult couplings. Furthermore, mechanistic investigations suggest a possible role of copper in the catalytic cycle...
  7. pmc T-type calcium channels regulate cortical plasticity in-vivo. [corrected]
    Victor N Uebele
    Department of Sleep Research, Merck Research Laboratories, Philadelphia, Pennsylvania, USA
    Neuroreport 20:257-62. 2009
    ..These results show that the T-type calcium channel plays a central role in cortical plasticity...
  8. ncbi request reprint Fluorescence resonance energy transfer (FRET) as a high-throughput assay for coupling reactions. Arylation of amines as a case study
    Shaun R Stauffer
    Department of Chemistry, Yale University, P O Box 208107, New Haven, Connecticut 06520 8107, USA
    J Am Chem Soc 125:6977-85. 2003
    ..Reactions with K(3)PO(4) base in aqueous mixtures of polar and nonpolar organic solvents were shown to be appropriate for the amination chemistry...
  9. ncbi request reprint Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid
    Matthew G Stanton
    J Med Chem 50:3431-3. 2007
    ....