Shaun R Stauffer
Affiliation: Merck Research Laboratories
- Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformationShaun R Stauffer
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 17:1788-92. 2007....
- Small molecule inhibition of the Bcl-X(L)-BH3 protein-protein interaction: proof-of-concept of an in vivo chemopotentiator ABT-737Shaun 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...
- Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretaseJames 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...
- Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sitesGeorgia 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...
- Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithromboticsJames 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...
- Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronatesJames 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...
- 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...
- Fluorescence resonance energy transfer (FRET) as a high-throughput assay for coupling reactions. Arylation of amines as a case studyShaun 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...
- Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloidMatthew G Stanton
J Med Chem 50:3431-3. 2007....