New 2-amino-thiazole-4-acetamides with antiplatelet activity

Archiv der Pharmazie
Klaus Rehse, Tobias Baselt

Abstract

In the Born test, 23 title compounds were synthesized and investigated for their antiplatelet activities against collagen, ADP, adrenaline, and platelet-activating factor (PAF) as inducers of the aggregation. Using collagen, three compounds with IC(50) values below 10 microM were found (3a, 3b, 3c) and 15 compounds with IC(50) values between 10 and 100 microM were determined. In general, a cyclohexylamino rest on an 4-carboxamide moiety is a pre-requisite for this pharmacological activity. A clear dependence from the substituent R(1) in the structural element Y is observed. The same is true for the spacer n in the 4-carboxamide substituent. Compound 3e showed strong ADP-antagonistic effects (IC(50) = 2.2 nM); 3c antagonized adrenaline (IC(50) = 2.8 nM), while 3n was highly effective against platelet-activating factor (IC(50) = 0.2 microM).

References

Dec 17, 2003·Archiv der Pharmazie·Matthias JohnsenErwin Bischoff
Mar 24, 2004·Archiv der Pharmazie·Anke Cwiklicki, Klaus Rehse
Jun 10, 2004·Archiv der Pharmazie·Ali Kemal YildizErwin Bischoff
Nov 11, 2005·Archiv der Pharmazie·Klaus Rehse, Jens Steege
Nov 11, 2005·Archiv der Pharmazie·Klaus Rehse, Hedwig Gonska
Feb 24, 2006·Archiv der Pharmazie·Katrin Märschenz, Klaus Rehse

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Citations

Apr 14, 2010·The American Journal of Forensic Medicine and Pathology·Tarin J RomichCharles A Catanese
Jul 10, 2010·Toxicology Mechanisms and Methods·R J Dinis-OliveiraT Magalhães
Jul 19, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·S V RajmaneP G More

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