Synthesis and in vitro study of platelet antiaggregant activity of some 4-quinazolinone derivatives.
Some new 4-quinazolinones were prepared. Their antiplatelet activity was evaluated in vitro with respect to aggregation induced by ADP, collagen, arachidonic acid and the platelet serotonin release reaction. Most molecules showed an inhibiting power similar to that of acetylsalicylic acid under the same conditions, and even greater when aggregation was induced by ADP. Reduction of the 4-quinazolinone derivatives to their 1,2,3,4-tetrahydroquinazoline homologues produced an increase in platelet inhibitory action except when ADP is the inductor.
Gravier
D
D
Laboratoire de Chimie Organique, INSERM Unité N. 8, Université de Bordeaux II, France.
Dupin
J P
JP
Casadebaig
F
F
Hou
G
G
Boisseau
M
M
Bernard
H
H
D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D009391:Nephelometry and Turbidimetry; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D012701:Serotonin / Q000378:metabolism
D010975:Platelet Aggregation Inhibitors; D011799:Quinazolines; D012701:Serotonin