title: Synthesis and bronchodilator activity of new quinazolin derivative.
abstract: Taking lead from a naturally occurring quinazolin vasicine, a number of compounds were developed and evaluated for bronchodilator and anti-allergic activities. One of these compounds was 2,4-diethoxy-6,7,8,9,10,12-hexahydroazepino[2,1-b]quinazolin-12-one, hereinafter named 95-4, exhibited marked bronchodilator activity evaluated on contracted trachea or constricted tracheo-bronchial tree. On intestinal smooth muscle too it showed relaxant effect. Tracheal relaxant effect was not found to be mediated through beta-adrenoceptors. Cumulative dose-response study with acetylcholine and histamine indicated for its non-specific direct effect on smooth muscles. 95-4 was found to be more potent than theophylline and less to that of salbutamol on dose basis. Tested by a number of experimental models, it was found devoid of anti-allergic activity. It was also found to be free from any adverse effect. 95-4 due to its marked bronchial muscle relaxant effect can find use in conditions associated with spasm of bronchial muscles.
authors.affiliation: Department of Pharmacology, Regional Research Laboratory (CSIR), Jammu, India. zabeer@rrljammu.org
authors.forename: A
authors.initials: A
authors.lastname: Zabeer
authors.forename: A
authors.initials: A
authors.lastname: Bhagat
authors.forename: O P
authors.initials: OP
authors.lastname: Gupta
authors.forename: G D
authors.initials: GD
authors.lastname: Singh
authors.forename: M S
authors.initials: MS
authors.lastname: Youssouf
authors.forename: K L
authors.initials: KL
authors.lastname: Dhar
authors.forename: O P
authors.initials: OP
authors.lastname: Suri
authors.forename: K A
authors.initials: KA
authors.lastname: Suri
authors.forename: N K
authors.initials: NK
authors.lastname: Satti
authors.forename: B D
authors.initials: BD
authors.lastname: Gupta
authors.forename: G N
authors.initials: GN
authors.lastname: Qazi
mesh_terms: D000470:Alkaloids / Q000138:chemical synthesis / Q000737:chemistry; D000818:Animals; D001381:Azepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: C513795:2,4-diethoxy-6,7,8,9,10,12-hexahydroazepino(2,1-b)quinazolin-12-one; D000470:Alkaloids; D001381:Azepines; D001993:Bronchodilator Agents; D011799:Quinazolines; C019592:vasicine