Zobrazeno 1 - 10
of 30
pro vyhledávání: '"G R Sitko"'
Autor:
G. R. Sitko, Maria S. Michener, Dietmar Seiffert, Madhu Chintala, Michael J. Forrest, Richard Raubertas, L. Alexandra Wickham, Tian-Quan Cai, Larry Handt
Publikováno v:
European Journal of Pharmacology. 758:107-114
Vorapaxar is a novel protease-activated receptor-1 (PAR-1) antagonist recently approved for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Patients who receiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::902413ed7bfb75c6fde7b750eac30399
https://doi.org/10.1016/j.ejphar.2015.03.073
https://doi.org/10.1016/j.ejphar.2015.03.073
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f489daa5ddd1907e6d600a79ad35db5d
https://doi.org/10.1016/j.bmcl.2007.11.050
https://doi.org/10.1016/j.bmcl.2007.11.050
Autor:
Bobby J. Lucas, Franklin C. Clayton, Daniel R. McMasters, James C. Barrow, Peter D. Williams, Robinson Kyle A, Theodore J. Detwiler, Yvonne M. Leonard, Sanderson Philip E, Julie A. Krueger, S. Dale Lewis, Rebecca B. White, Elizabeth A. Lyle, Cynthia Miller-Stein, William M. Sanders, Marie A. Holahan, Colleen M. McDonough, Youwei Yan, Jacquelynn J. Cook, Maria T. Stranieri, Joseph J. Lynch, Rominder Singh, G. R. Sitko, Lawrence Kuo, Terry A. Lyle, Craig A. Coburn, Zhongguo Chen, Dennis L. Bohn, Jules A. Shafer, Joseph P. Vacca, Audrey A. Wallace, Bruce D. Dorsey, Bradley K. Wong, Christopher S. Burgey, Stephen J. Gardell
Publikováno v:
Journal of Medicinal Chemistry. 46:461-473
Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b71ae0f7cadc2d662f0bc27e7e4d8c72
https://doi.org/10.1021/jm020311f
https://doi.org/10.1021/jm020311f
Autor:
Marie A. Holahan, Thomayant Prueksaritanont, E. L. Hand, Maria T. Stranieri, Jacquelynn J. Cook, G. R. Sitko, Joan D. Ellis
Publikováno v:
Biopharmaceutics & Drug Disposition. 18:649-663
Effects of pentobarbital on pharmacokinetics and pharmacodynamics of L-734,217, a potent fibrinogen receptor antagonist, were studied in male dogs. L-734,217 was given intravenously at 0.01 mg kg-1, in a cross-over fashion, to conscious dogs or to do
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1808a55120da1721a52aaf1e8a2e1807
https://doi.org/10.1002/(sici)1099-081x(199711)18:8<649::aid-bdd51>3.0.co
https://doi.org/10.1002/(sici)1099-081x(199711)18:8<649::aid-bdd51>3.0.co
Autor:
B. C. Askew, Thomayant Prueksaritanont, Joseph J. Lynch, Charles J. Mcintyre, Terrence G. Hamill, Rodney A. Bednar, Marie A. Holahan, Stanley L. Gaul, R. J. Lynch, G. R. Sitko, Robert J. Gould, Joan D. Glass, Cecila A. Hunt, John J. Baldwin, Jacquelynn J. Cook, Lynn M. Gorham, George D. Hartman, David A. Claremon, Maria T. Stranieri, Bohumil Bednar
Publikováno v:
Journal of Medicinal Chemistry. 40:1779-1788
The synthesis and pharmacological evaluation of 5 (L-738, 167), a potent, selective non-peptide fibrinogen receptor antagonist is reported. Compound 5 inhibited the aggregation of human gel-filtered platelets with an IC50 value of 8 nM and was found
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58d779663fd38db9ed7a212ced0cc2f2
https://doi.org/10.1021/jm9608117
https://doi.org/10.1021/jm9608117
Autor:
G. R. Sitko, Robert J. Gould, S. Lee Gaul, Guixiang Zhang, John D. Prugh, Bohumil Bednar, Maria T. Stranieri, Rodney A. Bednar, Marie A. Holahan, Jacquelynn J. Cook, George D. Hartman, R. J. Lynch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:865-870
Centrally constrained thieno[2,3- b ]thiophene sulfonamides have provided a potent, selective, orally active series of platelet aggregation inhibitors. Compound 21 showed excellent activity in the dog after a single oral dose of 200 μg/kg.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c0f8de86bc7089713bb925b1864d70c7
https://doi.org/10.1016/s0960-894x(97)00120-0
https://doi.org/10.1016/s0960-894x(97)00120-0
Autor:
R. J. Lynch, Rodney A. Bednar, Bohumil Bednar, Jacquelynn J. Cook, L.M. Vassallo, Marie A. Holahan, Stanley L. Gaul, Melissa S. Egbertson, Laura A. Libby, G. R. Sitko, Robert J. Gould, J.J. Lynch, George D. Hartman, Maria T. Stranieri
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2519-2524
Potency enhancing features of two series of fibrinogen receptor antagonists were combined to give analogs with improved potency and oral activity. Antagonists containing either alkyl or aryl sulfonamides and a central isoindolinone structural constra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::72ca48d34bf7bd0c8173abb3a1aecb0f
https://doi.org/10.1016/0960-894x(96)00473-8
https://doi.org/10.1016/0960-894x(96)00473-8
Autor:
Maria T. Stranieri, Wasyl Halczenko, R. J. Lynch, George D. Hartman, Joan D. Glass, John H. Hutchinson, Michael J. Breslin, G. R. Sitko, Marie A. Holahan, Robert J. Gould, Jacquelynn J. Cook, Karen M. Brashear
Publikováno v:
Journal of Medicinal Chemistry. 39:4583-4591
The structure-activity relationship of a series of orally active glycoprotein IIb/IIIa antagonists containing a nitrogen heterocycle grafted onto a 3,4-dihydro-1 (1H)-isoquinolinone core is described. These compounds are structurally novel analogs of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83f76a8016dbb8061d7260d25601263c
https://doi.org/10.1021/jm9604787
https://doi.org/10.1021/jm9604787
Publikováno v:
Thrombosis and Haemostasis. 74:640-645
SummaryThe antithrombotic efficacies of the coagulation factor Xa inhibitor recombinant tick anticoagulant peptide (rTAP) and heparin were compared in a canine model of left circumflex (LCX) coronary artery electrolytic lesion. Intravenous infusions
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ba12a327e87ae62f270984f67ca15cf6
https://doi.org/10.1055/s-0038-1649791
https://doi.org/10.1055/s-0038-1649791
Publikováno v:
Fibrinolysis. 7:195-202
Tick anticoagulant peptide (TAP) is a 60 amino acid protein originally isolated from the soft tick, Ornithodoros moubata, which exhibits potent anticoagulant properties due to its selective inhibition of blood coagulation factor Xa. We evaluated a re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8aab469769920f1c6294c69ff308031f
https://doi.org/10.1016/0268-9499(93)90021-m
https://doi.org/10.1016/0268-9499(93)90021-m