Author:
Sharma Mukesh C.,Kohli Dharm V.,
Abstract
Quantitative structure activity relationship analysis was performed on a series of thirty-three quinoline derivatives to establish the structural features required for angiotensin II receptor activity. QSAR models were derived by stepwise multiple regression analysis employing the method of least squares, using quantum chemical, thermodynamic, electronic and steric descriptors. Model showed best predictability of activity with cross validated value (q2 ) =0.7485, coeffi cient of determination (r2 ) =0.8734 and standard error of estimate (s) = 0.2690. These guidelines may be used to develop new antihypertensive agents based on the quinoline analogues scaffold.
Publisher
Indian Drug Manufacturers' Association (IDMA)
Subject
Drug Discovery,Pharmaceutical Science,Pharmacology
Reference11 articles.
1. 1. Timmermans P. B., Wong P. C., Chiu A. T., Herblin W.F., Benfield P., Carini D. J., Lee R. J., Wexler R. R., Saye J. A and Smith R. D.: Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev, 1993, 45(2),205-251
2. 2. Gasparo M de., Catt K J., T Inagami, Wright J.W and Unger.T.: International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev, 2000,52(3):415-472
3. 3. Kaschina E and Unger T.: Angiotensin AT1/AT2 receptors: regulation, signalling and function. Blood Press,2003, 12(2):70-88
4. 4. Catanzaro D.F., Mullins J.J and Morris B.J.: The biosynthetic pathway of renin in mouse submandibular gland. J Biol Chem, 1983, 258(12),7364-8
5. 5. Hadjipavlou-Litina D.: Review, reevaluation, and new results in quantitative structure-activity studies of anticonvulsants. Med Res Rev, 1998,18(2):91-119