4-(1H-pyrazol-1-yl)-2-butylamine derivatives as inhibitors of blood platelet aggregation.
Reaction of pyrazole and 3,5-dimethylpyrazole with methyl vinyl ketone gave 4-(1H-pyrazol-1-yl)-2-butanones which were converted to N-substituted 4-(1H-pyrazol-1-yl)-2-butylamines by reductive amination using ammonium acetate, primary or secondary amines and sodium cyanoborohydride as reducing agent. These new pyrazole derivatives were found to have an inhibitory effect on platelet aggregation in vitro.
Ferroni
R
R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Milani
L
L
Simoni
D
D
Orlandini
P
P
Guarneri
M
M
Franzé
D
D
Bardi
A
A
D000244:Adenosine Diphosphate / Q000494:pharmacology; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000494:pharmacology; D002082:Butylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D003094:Collagen / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001095:Arachidonic Acids; D002082:Butylamines; D010975:Platelet Aggregation Inhibitors; D011720:Pyrazoles; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen