Pyrido[2,3-d]pyrimidin-4(3H)-one derivatives and 1,2,3,4-tetrahydro- pyrido[2,3-d]pyrimidine derivatives: synthesis and in vitro study of their activity against platelet aggregation.
Some new derivatives of pyrido[2,3-d]pyrimidin-4(3H)-one A and 1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidines B were prepared. The study of their in vitro antiaggregating activity showed that the compounds A possessed an inhibitory potency when aggregation was induced with ADP. Their reduction to derivatives of 1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidine B led to a new series of molecules possessing a greater antiaggregating power. When compared to that of acetylsalicylic acid under the same conditions, this activity was weaker with collagen, the same with arachidonic acid-induced aggregation, but greater when aggregation was induced by ADP. However, they inhibited serotonin release only slightly. Compared to ginkgolide they remained weaker with PAF-induced aggregation.
Hou
G
G
Laboratoire de Chimie Organique, Université de Bordeaux II, France.
Gravier
D
D
Casadebaig
F
F
Dupin
J P
JP
Bernard
H
H
Boisseau
M
M
D016718:Arachidonic Acid / Q000494:pharmacology; D003094:Collagen / Q000494:pharmacology; D004224:Diterpenes; D005343:Fibrinolytic Agents / Q000494:pharmacology; D046934:Ginkgolides; D006801:Humans; D066298:In Vitro Techniques; D007783:Lactones / Q000494:pharmacology; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D012701:Serotonin / Q000097:blood; D013055:Spectrophotometry, Infrared
D004224:Diterpenes; D005343:Fibrinolytic Agents; D046934:Ginkgolides; D007783:Lactones; D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D011743:Pyrimidines; D011744:Pyrimidinones; D016718:Arachidonic Acid; D012701:Serotonin; D003094:Collagen; C045856:ginkgolide B