title: Progress in 5H[1]benzopyrano[4,3-d]pyrimidin-5-amine series: 2-methoxy derivatives effective as antiplatelet agents with analgesic activity.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Genova, Genoa, Italy. obruno@unige.it
authors.forename: Olga
authors.initials: O
authors.lastname: Bruno
authors.forename: Chiara
authors.initials: C
authors.lastname: Brullo
authors.forename: Silvia
authors.initials: S
authors.lastname: Schenone
authors.forename: Angelo
authors.initials: A
authors.lastname: Ranise
authors.forename: Francesco
authors.initials: F
authors.lastname: Bondavalli
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Barocelli
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Tognolini
authors.forename: Francesca
authors.initials: F
authors.lastname: Magnanini
authors.forename: Vigilio
authors.initials: V
authors.lastname: Ballabeni
mesh_terms: 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
chemical_list: D018712:Analgesics, Non-Narcotic; D010975:Platelet Aggregation Inhibitors; D011743:Pyrimidines; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen