SYNTHESIS, CHARACTERIZATION, BIOLOGICAL EVALUATION AND ADME STUDIES USING IN SILICO TECHNIQUES OF NOVEL DERIVATIVES OF BENZOTHIAZOLYL-AMIDES AS NON-ACIDIC ANTI-INFLAMMATORY AGENTSAbstract
Non-steroidal anti-inflammatory drugs (NSAIDs) have been used to treat various ailments for over 100 years. As a class, these drugs possess anti-inflammatory, anti-allergy, analgesic and antipyretic activity. A series of benzothiazolyl-amides has been synthesized and tested for anti-inflammatory activity. Basic NSAIDs are gaining interest because of their improved biological properties with the aim of improving the therapeutic index through prevention of gastrointestinal complications. The title compounds were identified by performing Thin Layer Chromatography and recording their physical constants. They were further characterized by spectral analysis (IR, 1HNMR, Mass spectroscopy). The effect of the synthesized compounds on inflammation, using the carageenan induced mouse paw edema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents. Anti-inflammatory activity was influenced by some structural characteristics of the synthesized compounds. Some physicochemical parameters and ADME Properties were computed by using software programs.
V. S. Velingkar*, D. C. Ahire, N. S. Kolhe, M.M. Shidore and G. Pokharna
Department of Pharmaceutical Chemistry, Principal K. M. Kundnani College of Pharmacy, Jote joy Bldg. Plot no. 23, Rambhau Salgaonkar Marg, Cuffe Parade, Colaba, Mumbai, Maharashtra, India
02 August, 2010
14 November, 2010
26 December, 2010
01 January, 2011