Výsledky vyhledávání - "T. G. Van Dinther"

Biological properties of synthetic glycoconjugate mimics of heparin comprising different molecular spacers

Autor: C.M. Dreef-Tromp, Jan E. M. Basten, C. A. A. Van Boeckel, M.A. Broekhoven, Petitou Maurice, T. G. Van Dinther

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 8:2081-2086

The in vitro antithrombotic activity of synthetic glycoconjugates I and II, comprising a flexible polyethylene glycol type and a rigid polyglucose type spacer, respectively, are compared to heparin.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d678228099851aff9ec3a8f0eaf8ebfd
https://doi.org/10.1016/s0960-894x(98)00382-5

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A cross-over comparison of the anti-clotting effects of three low molecular weight heparins and glycosaminoglycuronan

Autor: T. G. Van Dinther, A. F. Cohen, J. M. T. Van Griensven, J.C.J. Stiekema

Publikováno v: British Journal of Clinical Pharmacology. 36:51-56

1. The anti-clotting effects after intravenous administration of three low molecular weight (LMW) heparins, Fragmin (KABI 2165), Fraxiparine (CY 216), Clexane (PK 10169) and the LMW mixture of glycosaminoglycuronans Orgaran (Org 10172) were compared

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1162830ba0b5d5a965a85d2883191b3c
https://doi.org/10.1111/j.1365-2125.1993.tb05891.x

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ChemInform Abstract: 1-Aminoisoquinoline as Benzamidine Isoster in the Design and Synthesis of Orally Active Thrombin Inhibitors

Autor: Johannes Bernardus Maria Rewinkel, A. M. M. Rood, T. G. Van Dinther, A.J.S.M. Jenneboer, C. A. A. Van Boeckel, A. B. J. Noach, P. J. M. van Galen, Hans Lucas

Publikováno v: ChemInform. 30

Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::449d553a4ec8302d5299a2380c37132f
https://doi.org/10.1002/chin.199926205

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ChemInform Abstract: Design, Synthesis and Testing of Amino-Bicycloaryl Based Orally Bioavailable Thrombin Inhibitors

Autor: Hans Lucas, Johannes Bernardus Maria Rewinkel, A. B. J. Noach, A.J.S.M. Jenneboer, Martin J. Smit, T. G. Van Dinther, A. M. M. Rood, C. A. A. Van Boeckel

Publikováno v: ChemInform. 31

Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioav

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c1ceeaf121ec2f0565ef712f11bdfcad
https://doi.org/10.1002/chin.200005281

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Pharmacological Profile of the Chemically Synthesized Antithrombin III Binding Fragment of Heparin (Pentasaccharide) in Rats

Autor: T. G. Van Dinther, H. C. T. Moelker, C. A. A. Van Boeckel, D.G. Meuleman, P.M.J. Hobbelen, G.M.T. Vogel

Publikováno v: Thrombosis and Haemostasis. 63:265-270

SummaryThe antithrombotic and haemostatic effects of a pentasaccharide, the chemically synthesized antithrombin III (AT-III) binding fragment of heparin (PENTA), were investigated in rats in comparison with heparin. PENTA showed a dose-dependent anti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dafa28c50c51bda1ad18b7ecfab24685
https://doi.org/10.1055/s-0038-1645206

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Antithrombotic properties of a direct thrombin inhibitor with a prolonged half-life and AT-mediated factor Xa inhibitory activity

Autor: G.M.T. Vogel, Martin-Jan Smit, D.G. Meuleman, Rogier C. Buijsman, T. G. Van Dinther, A. W. M. Princen

Publikováno v: Journal of thrombosis and haemostasis : JTH. 1(9)

Rebound thrombin generation after successful thrombolysis might be related to (i) too short-term anticoagulant therapy and to (ii) the inability of heparin derivatives to inhibit clot-bound thrombin. To meet these shortcomings, a compound was synthes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f922721c8042188ad9abfa05c2906f69
https://pubmed.ncbi.nlm.nih.gov/12941035

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Pre-clinical pharmacological profile of the novel glycoconjugate Org 36764 with both factor Xa and thrombin (IIa) inhibitory activities

Autor: G M, Vogel, R G, van Amsterdam, T G, van Dinther, M, Tromp, D G, Meuleman

Publikováno v: Thrombosis and haemostasis. 84(4)

Org 36764, is an antithrombin III (AT) and thrombin binding carbohydrate, which accelerates the inactivation of both factor Xa and thrombin by AT. It displays in buffer an anti-Xa and anti-thrombin activity of 415 and 2 U/mg, respectively, compared t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2daa675c955a557defd4d4ce0805a1ed
https://pubmed.ncbi.nlm.nih.gov/11057859

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Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors

Autor: T. G. Van Dinther, A. M. M. Rood, Hans Lucas, Martin J. Smit, C. A. A. Van Boeckel, A. B. J. Noach, A.J.S.M. Jenneboer, Johannes Bernardus Maria Rewinkel

Publikováno v: Bioorganicmedicinal chemistry letters. 9(19)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6193e1539ec09580a2c261a2bd60c868
https://pubmed.ncbi.nlm.nih.gov/10522702

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1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors

Autor: A. M. M. Rood, P. J. M. van Galen, Hans Lucas, C. A. A. Van Boeckel, T. G. Van Dinther, A. B. J. Noach, Johannes Bernardus Maria Rewinkel, A.J.S.M. Jenneboer

Publikováno v: Bioorganic and Medicinal Chemistry Letters, 9(5), 685-690. Elsevier

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bd8f76df225f624227fa8cfd1f8b41c
https://pubmed.ncbi.nlm.nih.gov/10201829

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Feasible synthesis and biological properties of six 'non-glycosamino' glycan analogues of the antithrombin III binding heparin pentasaccharide

Autor: Jan B. L. Damm, Hans Lucas, Jan E. M. Basten, A. M. M. Rood, M.A. Broekhoven, P. Westerduin, A. Visser, H. van der Heijden, G.T. Overklift, T. G. Van Dinther, C. A. A. Van Boeckel, D.G. Meuleman, R. G. M. Van Amsterdam, G.M.T. Vogel

Publikováno v: Bioorganicmedicinal chemistry. 2(11)

In this paper, we report the synthesis of ‘non-glycosamino’ glycan analogues 5–10 of the antithrombin III binding pentasaccharide 1 . Pentasaccharides 5–10 feature a pseudo-alternating EFGH tetrasaccharide sequence, that is, the disaccharide

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0845afdc2350e532cdb06e357d415c5
https://pubmed.ncbi.nlm.nih.gov/7757423

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