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Journal of Pharmacology and Toxicology
Year: 2007  |  Volume: 2  |  Issue: 3  |  Page No.: 271 - 277

Synthesis, Biological Evaluation and QSPR Studies ofAmino Acid Conjugates of Cinmetacin

C.M. Lucksha, D. Agarwal, N.S.H.N. Moorthy, C. Karthikeyan and P. Trivedi    

Abstract: Synthesis and biological evaluation of amino acid conjugates of cinmetacin was carried out to improve some pharmacokinetic properties and to minimize some undesirable side effects (especially ulcerogenic effect). Dissolution studies and hydrolysis studies on simulated intestinal fluid (pH 7.4) follow the first order kinetics. The quantitative structure property relationship studies reveals that rate of hydrolysis of the compounds is inversely related to partition coefficient values. The study of acute and chronic anti-inflammatory and ulcerogenic activity gave statistically significant results and it concluded that the compounds minimize the gastric side effects of cinmetacin remarkably.

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