Synthesis and bronchodilator activity of new quinazolin derivative.
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.
Zabeer
A
A
Department of Pharmacology, Regional Research Laboratory (CSIR), Jammu, India. zabeer@rrljammu.org
Bhagat
A
A
Gupta
O P
OP
Singh
G D
GD
Youssouf
M S
MS
Dhar
K L
KL
Suri
O P
OP
Suri
K A
KA
Satti
N K
NK
Gupta
B D
BD
Qazi
G N
GN
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
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