Výsledky vyhledávání - "Peter D. Winocour"

In Vitro and in Vivo Properties of Bicyclic Lactam Inhibitors

Autor: Lorraine Leblond, B. Grouix, C. Boudreau, M.A. Siddiqui, Peter D. Winocour, Q. Yang

Publikováno v: Thrombosis Research. 100:195-209

We have developed potent and selective thrombin inhibitors with a novel non-peptidic structure. A bicyclic lactam was used as the scaffold on which various P1 and P3 motifs were substituted. Herein, we report the in vitro and in vivo properties of fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6aaa9e39e347aa7ad1c550c3e8761de4
https://doi.org/10.1016/s0049-3848(00)00333-9

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Incorporation of an Asp-Ser Sequence to Form an RGDS-like Motif in Hirutonin

Autor: Maria I.C. Gyongyossy-Issa, Lorraine Leblond, Veronica van Wyk, Dana V. Devine, Peter D. Winocour

Publikováno v: Thrombosis Research. 99:343-352

We investigated the effect on in vitro platelet function of hirutonin, a modified hirutonin with an RGD-like motif, a pseudo-RGDS peptide and a linear RGDS peptide. Inhibition of expression of surface fibrinogen on ADP-activated platelets with 40 μM

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::451ba48536e830298ab7be3935ba5f54
https://doi.org/10.1016/s0049-3848(00)00257-7

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Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1′ modifications

Autor: A. Susser, Peter D. Winocour, John DiMaio, Debra R. Holland, M. Arshad Siddiqui, Kent A. Berryman, Sophie Levesque, Janet S. Plummer, D. Lafleur, Jeremy J. Edmunds, Scott R. Eaton, J. Ronald Rubin, Annette Marian Doherty, Cuiman Cai, Wayne L. Cody, Stephen T. Rapundalo, Lakshmi S. Narasimhan, Yves St-Denis

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:835-840

The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors are described. We have explored the SAR around the P1' site. Modification of the P1' site has been found to affect potency and selectivity.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f3fd52bd5a522c0e984c8c93c262c0d
https://doi.org/10.1016/s0960-894x(99)00096-7

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[Untitled]

Autor: Peter D. Winocour, Paul L. Juneau, Kim P. Gallagher, Carolyn Finkle, Diane P. Ignasiak, Thomas B. McClanahan

Publikováno v: Journal of Thrombosis and Thrombolysis. 7:301-306

Deep venous thrombosis (DVT) is a common cardiovascular disease, resulting in significant mortality each year in the United States. Direct thrombin inhibitors represent a new class of drugs that could potentially be better than conventional antithrom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1acba6f879a541dc4cd46d139f033924
https://doi.org/10.1023/a:1008987211850

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Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 Modifications

Autor: J. Ronald Rubin, Darin R. Kent, Debra R. Holland, John DiMaio, Yves St-Denis, Annette Marian Doherty, Sophie Levesque, Cuiman Cai, Peter D. Winocour, Jeremy J. Edmunds, M. Arshad Siddiqui, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Janet S. Plummer, John X. He, Alan J. Susser, Kent A. Berryman, Wayne L. Cody

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:3409-3414

The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selectiv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3535a23a3fd9399e06e71180b3a6ca9
https://doi.org/10.1016/s0960-894x(98)00613-1

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Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications

Autor: Sophie Levesque, Kent A. Berryman, M. Arshad Siddiqui, Jeremy J. Edmunds, Peter D. Winocour, John DiMaio, Annette Marian Doherty, Yves St-Denis, C.E. Augelli-Szafran, Benoit Bachand, Lorraine Leblond, Lakshmi S. Narasimhan, J. Ronald Rubin, Micheline Tarazi, J.R. Penvose-Yi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:3193-3198

Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting ph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::197b252f0565e168178e927f9b2d1654
https://doi.org/10.1016/s0960-894x(98)00550-2

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BCH-2763, a Novel Potent Parenteral Thrombin Inhibitor, Is an Effective Antithrombotic Agent in Rodent Models of Arterial and Venous Thrombosis – Comparisons with Heparin, r-Hirudin, Hirulog, Inogatran and Argatroban

Autor: Annie St. Pierre, Lorraine Leblond, Carolyn D. Finkle, Peter D. Winocour, Isabelle Deschenes, Dimaio John

Publikováno v: Thrombosis and Haemostasis. 79:431-438

SummaryCurrent clinical use of heparin as an antithrombotic agent is limited by suboptimal efficacy and safety considerations. Thrombin’s central role in thrombosis makes it an attractive target to develop more effective and safer antithrombotic ag

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c7817d15c6bcf7c2c43c755b1abdbce8
https://doi.org/10.1055/s-0037-1615003

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Effective Use of BCH-2763, a New Potent Injectable Direct Thrombin Inhibitor, in Combination with Tissue Plasminogen Activator (tPA) in a Rat Arterial Thrombolysis Model

Autor: Carolyn D. Finkle, Isabelle Deschenes, Peter D. Winocour

Publikováno v: Thrombosis and Haemostasis. 80:186-191

SummaryCurrent therapeutic use of heparin as an adjunct to thrombolytic therapy for myocardial infarction is suboptimal with respect to efficacy and bleeding risk. In a rat carotid arterial thrombolysis model (FeCl3-induced injury) we evaluated the c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::eb4e9e6034c57098971e67d1efb85418
https://doi.org/10.1055/s-0037-1615161

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ChemInform Abstract: Novel Bicyclic Lactam Inhibitors of Thrombin: Potency and Selectivity Optimization Through P1 Residues

Autor: Peter D. Winocour, Patrice Preville, M. Arshad Siddiqui, Yves St-Denis, Benoit Bachand, Jeremy J. Edmunds, Sophie Levesque, John R. Rubin, Lorraine Leblond

Publikováno v: ChemInform. 33

Peptidomimetic inhibitors of thrombin lacking the important Ser195–carbonyl interaction have been prepared. The binding energy lost after the removal of the activated carbonyl was recaptured through a series of modifications of the P1 residues of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ea8fc7884504ed58a4da56e6c2d73b6c
https://doi.org/10.1002/chin.200210140

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ChemInform Abstract: Novel Bicyclic Lactam Inhibitors of Thrombin: Highly Potent and Selective Inhibitors

Autor: Lorraine Leblond, Sophie Levesque, Benoit Bachand, Jeremy J. Edmunds, Micheline Tarazi, Peter D. Winocour, Patrice Preville, Yves St-Denis, M. Arshad Siddiqui

Publikováno v: ChemInform. 33

The potency and selectivity of a previous series of low molecular weight thrombin inhibitors were improved through modifications of the P1 and P3 residues. Introduction of diphenyl substituted sulfonamides in the P3 moiety led to highly efficacious c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::42f8ab8d99c550bf6b0e262b2428609b
https://doi.org/10.1002/chin.200232244

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