title: New 1H-pyrazole-4-carboxamides with antiplatelet activity.
abstract: 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).
authors.affiliation: Institut für Pharmazie, Freie Universität Berlin, Berlin, Germany. rehiwer@zedat.fu-berlin.de
authors.forename: Klaus
authors.initials: K
authors.lastname: Rehse
authors.forename: Joscha
authors.initials: J
authors.lastname: Kotthaus
authors.forename: Laleh
authors.initials: L
authors.lastname: Khadembashi
mesh_terms: 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
chemical_list: D000577:Amides; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D000244:Adenosine Diphosphate; D004837:Epinephrine