Synthesis of 6-[(4-imidazol-1-yl)-phenyl]-4-phenyl 4,5-dihydro-2H-pyridazin-3-one: a potential blood platelet aggregation inhibitor.
A new 4,5 diaryl pyridazin-3-one, an analogue of imazodan and Cl-930 was prepared starting from conveniently available chalcone. The resulting derivative was tested in order to determine the area of pharmacological activity. This compound was devoid of positive inotropic effects but showed an important inhibition of PAF-acether induced blood platelet aggregation in vitro with a Cl50 value of 3,4 microM. Ex vivo, anti-aggregating effect against PAF-acether was less important with a DE50 value of 63 mg/kg per os.
Coudert
P
P
Groupe de Recherche en Pharmacochimie, Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Clermont-Ferrand.
Rubat
C
C
Couquelet
J
J
Tronche
P
P
D000818:Animals; D004285:Dogs; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology
D010975:Platelet Aggregation Inhibitors; D011724:Pyridazines; C065810:6-((4-imidazol-1-yl)phenyl)-4-phenyl-4,5-dihydro-2H-pyridazin-3-one