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Synthesis and bronchodilator activity of new quinazolin derivative

IR@CSIR-IIIM

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Title Synthesis and bronchodilator activity of new quinazolin derivative
 
Creator Ahmed, Zabeer
Bhagat, A.
Gupta, O.P.
Singh, G.D.
Youssouf, M.S.
Dhar, K.L.
Suri, O.P.
Suri, K.A.
Satti, N.K.
Gupta, B.D.
Qazi, G.N.
 
Subject Chemical Sciences
Pharmacological Sciences
 
Description 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 β-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.
 
Date 2006
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://iiim.csircentral.net/352/1/10.1016j.ejmech.2005.09.010.pdf
Ahmed, Zabeer and Bhagat, A. and Gupta, O.P. and Singh, G.D. and Youssouf, M.S. and Dhar, K.L. and Suri, O.P. and Suri, K.A. and Satti, N.K. and Gupta, B.D. and Qazi, G.N. (2006) Synthesis and bronchodilator activity of new quinazolin derivative. European Journal of Medicinal Chemistry, 41 (3). pp. 429-434. ISSN 02235234
 
Relation http://dx.doi.org/10.1016/j.ejmech.2005.09.010
http://iiim.csircentral.net/352/