1093729-21-5Relevant articles and documents
New 2-amino-thiazole-4-acetamides with antiplatelet activity
Rehse, Klaus,Baselt, Tobias
experimental part, p. 645 - 654 (2009/04/06)
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 IC50 values below 10 μM were found (3a, 3b, 3c) and 15 compounds with IC50 values between 10 and 100 μM 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 R1 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 (IC50 = 2.2 nM); 3c antagonized adrenaline (IC50 = 2.8 nM), while 3n was highly effective against platelet-activating factor (IC50 = 0.2 μM).