title: Synthesis and pharmacological evaluation of 2,5-cycloamino-5H-[1]benzopyrano[4,3-d]pyrimidines endowed with in vitro antiplatelet activity.
abstract: A series of new 2,5-cycloamino-5H-[1]benzopyrano[4,3-d]pyrimidines 3a-i have been synthesized and tested in vivo for the anti-inflammatory/analgesic/antipyretic effects and in vitro to evaluate the antiplatelet activity on guinea-pig platelet-rich plasma aggregated by collagen, adenosine-5'-diphosphate (ADP) and arachidonic acid (AA). Title compounds were ineffective in vivo; however, the pyrrolidino derivatives 3a and 3c exhibited an antiplatelet activity against all the aggregants differing from that of acetylsalicylic acid (ASA) while the 5-morpholino derivatives 3g-i showed the most potent ASA-like antiplatelet activity.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi, Viale Benedetto XV, 3-16132, Genova, Italy. obruno@unige.it
authors.forename: O
authors.initials: O
authors.lastname: Bruno
authors.forename: C
authors.initials: C
authors.lastname: Brullo
authors.forename: A
authors.initials: A
authors.lastname: Ranise
authors.forename: S
authors.initials: S
authors.lastname: Schenone
authors.forename: F
authors.initials: F
authors.lastname: Bondavalli
authors.forename: E
authors.initials: E
authors.lastname: Barocelli
authors.forename: V
authors.initials: V
authors.lastname: Ballabeni
authors.forename: M
authors.initials: M
authors.lastname: Chiavarini
authors.forename: M
authors.initials: M
authors.lastname: Tognolini
authors.forename: M
authors.initials: M
authors.lastname: Impicciatore
mesh_terms: D000244:Adenosine Diphosphate / Q000378:metabolism; D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D016718:Arachidonic Acid / Q000378:metabolism; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D003094:Collagen / Q000378:metabolism; D004195:Disease Models, Animal; D004487:Edema / Q000188:drug therapy; D006168:Guinea Pigs; D010146:Pain / Q000188:drug therapy; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D001578:Benzopyrans; D010975:Platelet Aggregation Inhibitors; D011743:Pyrimidines; D016718:Arachidonic Acid; D000244:Adenosine Diphosphate; D003094:Collagen