title: Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation.
abstract: In pursuing our research on some 2,4-diamino-benzopyranopyrimidines and 2-amino-5,6-dihydrobenzo[h]quinazolines, previously reported as antiplatelet and analgesic/anti-inflammatory agents respectively, we designed and synthesized a new series of 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted. The insertion of amino substituents at positions 2 and 4 of the benzoquinazoline scaffold resulted in compounds endowed with a potent ASA-like antiplatelet activity, combined with an anti-inflammatory activity comparable, in some cases, to that of indomethacin, used as a reference drug.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, University of Genoa, V.le Benedetto XV, 3-16132 Genova, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Brullo
authors.forename: Massimo
authors.initials: M
authors.lastname: Rocca
authors.forename: Paola
authors.initials: P
authors.lastname: Fossa
authors.forename: Elena
authors.initials: E
authors.lastname: Cichero
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Barocelli
authors.forename: Vigilio
authors.initials: V
authors.lastname: Ballabeni
authors.forename: Lisa
authors.initials: L
authors.lastname: Flammini
authors.forename: Carmine
authors.initials: C
authors.lastname: Giorgio
authors.forename: Francesca
authors.initials: F
authors.lastname: Saccani
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Domenichini
authors.forename: Olga
authors.initials: O
authors.lastname: Bruno
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004487:Edema / Q000188:drug therapy*; D006168:Guinea Pigs; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D011743:Pyrimidines; D011799:Quinazolines; D011451:Prostaglandin-Endoperoxide Synthases