Amidino-Containing Schiff Base Copper(II) and Iron(III) Chelates as a Thrombin Inhibitor

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Synthesis and evaluation of guanidine-containing Schiff base copper(II), zinc(II), and iron(III) chelates as trypsin inhibitors.

3-Formyl-4-hydroxyphenylguanidine hydrochloride and its Schiff base copper(II), zinc(II), and iron(III) chelates were synthesized and their inhibitory activity against bovine beta-trypsin were determined. Syntheses of Schiff base metal chelates were carried out from 3-formyl-4-hydroxyphenylguanidine, various L-amino acids, and divalent metal acetate. Their structures were established on the bas...

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Chem. Pharm. Bull. 53(1) 22—26 (2005)

critical role in the blood coagulation cascade. Thrombin converts fibrinogen into fibrin which forms part of the blood clot, and activates other blood coagulation factors such as V, VIII, XIII, and protein C. Moreover, thrombin also activates blood platelets, and acts as a mitogen for various cell types. Thus, thrombin has become a special target in the design and development of antithrombotic ...

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Synthesis and Thrombin, Factor Xa and U46619 Inhibitory Effects of Non-Amidino and Amidino N2-Thiophenecarbonyl- and N2-Tosylanthranilamides

Thrombin (factor IIa) and factor Xa (FXa) are key enzymes at the junction of the intrinsic and extrinsic coagulation pathways and are the most attractive pharmacological targets for the development of novel anticoagulants. Twenty non-amidino N²-thiophencarbonyl- and N²-tosyl anthranilamides 1-20 and six amidino N²-thiophencarbonyl- and N²-tosylanthranilamides 21-26 were synthesized to evaluate ...

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ژورنال

عنوان ژورنال: Chemical and Pharmaceutical Bulletin

سال: 2005

ISSN: 0009-2363,1347-5223

DOI: 10.1248/cpb.53.22