New 1H-pyrazole-4-carboxamides with antiplatelet activity.
Nine title compounds were synthesized and investigated in the Born test 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 100 microM were found (3b, 3e, 3i). Activities in nanomolar concentrations were observed against ADP (3b, IC50 = 9.4 nM), adrenaline (3i, IC50 = 5.8 nM), and platelet activating factor (3e, IC50 = 0.45 nM).
Rehse
Klaus
K
Institut für Pharmazie, Freie Universität Berlin, Berlin, Germany. rehiwer@zedat.fu-berlin.de
Kotthaus
Joscha
J
Khadembashi
Laleh
L
D000244:Adenosine Diphosphate / Q000494:pharmacology; D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002478:Cells, Cultured; D004837:Epinephrine / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D010972:Platelet Activating Factor / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000577:Amides; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D000244:Adenosine Diphosphate; D004837:Epinephrine