Progress in 5H[1]benzopyrano[4,3-d]pyrimidin-5-amine series: 2-methoxy derivatives effective as antiplatelet agents with analgesic activity.
A series of 2-methoxy-5H[1]benzopyrano[4,3-d]pyrimidin-5-amines were prepared and screened for their in vitro antiplatelet activity inducing the aggregation by ADP, arachidonic acid (AA) and collagen. In vivo experiments were performed in order to evaluate their antiphlogistic, analgesic and antipyretic activities. Title compounds showed antiplatelet activity in aggregation AA or collagen-induced, and a good analgesic activity without any gastric toxicity. Comparison with a number of analogue benzopyrano[4,3-d]pyrimidine derivatives and some SAR consideration were reported.
Bruno
Olga
O
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Genova, Genoa, Italy. obruno@unige.it
Brullo
Chiara
C
Schenone
Silvia
S
Ranise
Angelo
A
Bondavalli
Francesco
F
Barocelli
Elisabetta
E
Tognolini
Massimiliano
M
Magnanini
Francesca
F
Ballabeni
Vigilio
V
D000244:Adenosine Diphosphate; D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D016718:Arachidonic Acid; D003094:Collagen; D005753:Gastric Mucosa / Q000187:drug effects; D006168:Guinea Pigs; D051379:Mice; D010147:Pain Measurement; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D010975:Platelet Aggregation Inhibitors; D011743:Pyrimidines; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen