Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Rhonda M Lachance"'
Autor:
Rhonda M Lachance, Stephen R. Rapp, John J. Parlow, Peter Harris, Rita M. Huff, Case Brenda, Mary W. Burney, Thomas J. Girard, Deborah A. Mischke, Ennis Michael D, Rhonda S. Woerndle, Kerri A. Hall, Ronald R. Hiebsch
Publikováno v:
Journal of Medicinal Chemistry. 53:2010-2037
Polymer-assisted solution-phase (PASP) parallel library synthesis was used to discover a piperazinyl glutamate pyridine as a P2Y(12) antagonist. Exploitation of this lead provided compounds with excellent inhibition of platelet aggregation as measure
Autor:
John J, Parlow, Mary W, Burney, Brenda L, Case, Thomas J, Girard, Kerri A, Hall, Peter K, Harris, Ronald R, Hiebsch, Rita M, Huff, Rhonda M, Lachance, Deborah A, Mischke, Stephen R, Rapp, Rhonda S, Woerndle, Michael D, Ennis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1388-1394
Efforts to refine the SAR of the piperazinyl-glutamate-pyridines for more potent analogs with improved pharmacokinetic profiles are described. Exploring substituted piperidines and other ring systems at the 4-pyridyl position led to compounds with im
Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation
Autor:
Kerri A. Hall, Rita M. Huff, Rhonda M. Lachance, Ennis Michael D, Rhonda S. Woerndle, Ronald R. Hiebsch, John J. Parlow, Stephen R. Rapp, Deborah A. Mischke, Brenda L. Case, Mary W. Burney, Thomas J. Girard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6148-6156
Piperazinyl-glutamate-pyrimidines were prepared with oxygen, nitrogen, and sulfur substitution at the 4-position of the pyrimidine leading to highly potent P2Y 12 antagonists. In particular, 4-substituted piperidine-4-pyrimidines provided compounds w
Autor:
Hayat K. Rahman, Tenbrink Ruth E, Barbara A. Schweitzer, Rita M. Huff, Steven W. Kortum, Gopichand Yalamanchili, Rhonda M. Lachance, Ennis Michael D
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5919-5923
Herein we describe the design and synthesis of a novel series of potent thienopyrimidine P2Y12 inhibitors and the negative impact protein binding has on the inhibition of platelet aggregation.
Publikováno v:
Journal of Thrombosis and Thrombolysis. 14:113-121
The Tissue Factor/Factor VIIa (TF/FVIIa) complex is an attractive target for pharmacological interruption of thrombin generation and hence blood coagulation, as this complex is the initiation point of the extrinsic pathway of coagulation. TF is a cel
Autor:
Peter Harris, Kerri A. Hall, Mary W. Burney, Thomas J. Girard, Stephen R. Rapp, Rita M. Huff, Ronald R. Hiebsch, Rhonda M Lachance, Case Brenda, Ennis Michael D, Rhonda S. Woerndle, Deborah A. Mischke, John J. Parlow
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
Polymer-assisted solution-phase (PASP) parallel library synthesis was used to discover a piperazinyl glutamate pyridine as a P2Y12 antagonist. Exploitation of this lead provided compounds with excellent inhibition of platelet aggregation as measured
Autor:
William C. Stallings, Ravi G. Kurumbail, Rhonda M Lachance, Anna M. Stevens, Roderick A Stegeman, Michael S. South, John J. Parlow, Thomas J. Girard, Dice Tom
Publikováno v:
Journal of medicinal chemistry. 46(19)
A solution-phase synthesis of an alpha-ketothiazole library of the general form D-Phe-L-AA-Arg-alpha-ketothiazole is described. The five-step synthesis is accomplished using a combination of polymeric reagents and polymer-assisted solution-phase puri
Autor:
Roderick A Stegeman, Ricky L. Fenton, William L. Neumann, Wood Rhonda, John J. Parlow, Ravi G. Kurumbail, Nancy S. Nicholson, Darin E. Jones, Michael S. South, Anna M. Stevens, Rhonda M Lachance, Thomas J. Girard, Michael Clare, William C. Stallings, Dice Tom, Case Brenda, Hayes Michael J
Publikováno v:
Journal of medicinal chemistry. 46(19)
Structure-based drug design (SBDD) and polymer-assisted solution-phase (PASP) library synthesis were used to develop a series of pyrazinone inhibitors of the Tissue Factor/Factor VIIa (TF/VIIa) complex. The crystal structure of a tripeptide-alpha-ket
Autor:
James A. Szalony, Wood Rhonda, Nancy S. Nicholson, John J. Parlow, Rhonda M Lachance, Osman D. Suleymanov, South Michael S, Anita K. Salyers
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 306(3)
This study was designed to evaluate the antithrombotic efficacy and bleeding propensity of a selective, small-molecule inhibitor of tissue factor/factor VIIa (TF/VIIa) in comparison to small-molecule, selective inhibitors of factor Xa and thrombin in
Autor:
Darin E. Jones, Hayes Michael J, Rhonda M Lachance, Michael Clare, Wood Rhonda, Ravi G. Kurumbail, Nancy S. Nicholson, John J. Parlow, Roderick A Stegeman, Case Brenda, Thomas J. Girard, Michael S. South, Anna M. Stevens, William C. Stallings
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(14)
Structure-based drug design coupled with polymer-assisted solution-phase library synthesis was utilized to develop a series of pyrazinone inhibitors of the tissue factor/Factor VIIa complex. The crystal structure of a tri-peptide ketothiazole complex