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[email protected] The Open Conference Proceedings Journal, 2013, 4, 99-112
99
Open Access
Synthesis, Biological Activity, Molecular Modelling Studies and 3D-QSAR Investigations of N-[2-(aryl/substituted aryl)-4-oxo-1, 3-thiazolidin-3-yl] pyridine-4-carboxamides Asha B. Thomasa,*, Rabindra K. Nandaa, Lata P. Kothapallia, Piyush A. Sharmab and Kishori G. Aptec a
Department of Pharmaceutical Chemistry, Padm. Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pune, Maharashtra, India b
Department of Pharmaceutical Chemistry, Sri Aurobindo Institute of Pharmacy, Indore, Madhya Pradesh, India
c
National Toxicology Centre (NTC), Pune, Maharashtra, India Abstract: In the present research work new 4-thiazolidinones possessing dual cyclooxygenase/lipoxygenase inhibition were synthesized. Sixteen N-[2-(aryl/substitutedaryl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide derivatives(5a-q) differing by the phenyl group substitution were synthesized by sonication. Compounds N-[2-(4-chlorophenyl)-4-oxo-1, 3thiazolidin-3-yl] pyridine-4-carboxamide (5d) and N-[2-(4-nitrophenyl)-4-oxo-1, 3-thiazolidin-3-yl] pyridine-4-carboxamide (5f) showed promising anti-inflammatory activity investigated by the carrageenan induced edema model in rats. Compound 5f, was the most active in the series with low ulcerogenic index and good safety profile with highest in vitro inhibition of COX-1/COX-2 (89.28; 52.80%, p
