Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Cynthia L. Burns-Kurtis"'
Autor:
Stefan Senger, Máire A. Convery, Robert J. Young, Stephanie Irvine, Iain M. McLay, Robert I. West, David J. Belton, Savvas Kleanthous, Carl Adams, John R. Toomey, Anne M. Exall, Anthony J. Pateman, Theresa J. Roethke, Caroline M. Whittaker, Laiq Chaudry, David E. Davies, Angela Patikis, Cynthia L. Burns-Kurtis, Nigel S. Watson, Gary J. Stelman, David W. Brown, John D. Harling, Wendy R. Irving, Chuen Chan, Ping Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1588-1592
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the
Autor:
Shobha Senadhi, Joseph P. Marino, Cynthia L. Burns-Kurtis, Lorena A. Kallal, Dwight M. Morrow, Reema K. Thalji, Nambi Aiyar, Joseph A. Erhardt, Elizabeth A. Davenport
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4104-4107
Benzofuran-substituted urea analogs have been identified as novel P2Y1 receptor antagonists. Structure–activity relationship studies around the urea and the benzofuran moieties resulted in compounds having improved potency. Several analogs were sho
Autor:
Savvas Kleanthous, Alan D. Borthwick, David Brown, Cynthia L. Burns-Kurtis, Matthew Campbell, Laiq Chaudry, Chuen Chan, Marie-Olive Clarte, Máire A. Convery, John D. Harling, Eric Hortense, Wendy R. Irving, Stephanie Irvine, Anthony J. Pateman, Angela N. Patikis, Ivan L. Pinto, Derek R. Pollard, Theresa J. Roethka, Stefan Senger, Gita P. Shah, Gary J. Stelman, John R. Toomey, Nigel S. Watson, Robert I. West, Caroline Whittaker, Ping Zhou, Robert J. Young
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:618-622
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa inhibitors, incorporating neutral and basic monoaryl P4 groups, ultimately producing potent inhibitors with effective levels of ant
Autor:
Elizabeth A. Davenport, Reema K. Thalji, Nambi Aiyar, Todd L. Graybill, Peng Li, Allyn T. Londregan, Dwight M. Morrow, Angel I. Morales-Ramos, Terry Kiesow, Steve Zhao, John S. Mecom, Shobha Senadhi, Gregory D. Brown, Lorena A. Kallal, Beth Anne Knapp-Reed, Joseph P. Marino, Cynthia L. Burns-Kurtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:6222-6226
High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 328:231-239
Epoxy- and dihydroxy-eicosatrienoic acids (EETs and DHETs) are vasoactive cytochrome P450 metabolites of arachidonic acid. Interestingly, however, the mechanism(s) by which EETs/DHETs mediate smooth muscle relaxation remains unclear. In contrast to p
Autor:
Anthony J. Pateman, John R. Toomey, Paul F. Koster, Augustin Amour, Saul Needle, Laiq Chaudry, Melanie A Abboud, Champa Patel, Angela Patikis, Cynthia L. Burns-Kurtis, Robert J. Young, Richard E. Valocik, David Brown, Ping Zhou, Chuen Chan, Nigel S. Watson
Publikováno v:
Journal of Cardiovascular Pharmacology. 52:66-71
Background: Factor Xa (FXa) has been a target of considerable interest for drug development efforts aimed at suppressing thrombosis. In this report, a new orally active, small molecule, active-site directed FXa inhibitor, GW813893, has been profiled
Autor:
Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:28-33
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activitie
Autor:
Robert J. Young, David W. Brown, Stefan Senger, Chuen Chan, Máire A. Convery, Anthony J. Pateman, Nigel S. Watson, John R. Toomey, Ping Zhou, Henry Anderson Kelly, Shah Gita Punjabhai, Julia A. Hubbard, Angela Patikis, Cynthia L. Burns-Kurtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2927-2930
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhib
Autor:
Terry P. Kenakin, David W. Gray, Jim Coote, Alan Wise, Heather Giles, Cynthia L. Burns-Kurtis, Sara Pritchard, Noel Lloyd Staton, Jason D. Brown, Richard J. Wilson, Valerie Morrison, Susan Roomans, Sharron A. Rhodes, Kerri Ann Cartwright, Gerard Martin Paul Giblin, Jannatara Chowdhury, Vanessa J. Shield
Publikováno v:
British Journal of Pharmacology. 148:326-339
1. N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl}benzene sulphonamide (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity. 2. At r
Autor:
Cynthia L. Burns-Kurtis, Josephine H. Fox, Saul Needle, Elizabeth A. Capper, Anne M. Romanic, Alan R. Olzinski, Michael S. McQueney, Fiona M. Kelly
Publikováno v:
Cardiovascular Research. 62:610-620
Objective: Neointimal development following balloon angioplasty involves many factors including smooth muscle cell (SMC) migration and proliferation and extracellular matrix (ECM) remodeling. Further, in hypercholesterolemic (HC) conditions, there is