Abstract
A series of substituted thiazole derivatives (6–16) were synthesized to obtain new compounds with potential anti-inflammatory and analgesic activities. At equimolar oral doses, compounds 3-(piperidin-1-yl-methyl)-1, 3, 4-oxadiazol-2-thione (14), 5-amino-4-ethyl ester pyrazole (15), and 5-amino-3-phenylpyrazole derivatives (16) displayed anti-inflammatory and analgesic activities significant to those of diclofenac sodium in the carrageenan-induced paw edema test in rat and acetic acid-induced writhing test in mice,-respectively. The most active members of the series (9, 11, 14, 15, and 16) were selected for ulcerogenic potential study. These compounds exhibited quite less ulcerogenic index in the range of 0.44 to 0.62 whereas diclofenac sodium showed 4.67. The docking study results also indicated that the compound 6, 7, 8, 11, and 14 exhibited the docking score ranging from −3.951 to −4.691.
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Acknowledgments
The authors are wholeheartedly grateful to Prof. T. J. Sawant, Founder Secretary, Jayawant Sikshan Prasarak Mandal’s, Charak College of Pharmacy and Research, Wagholi, Pune for encouragements and support. Mr. Rishikesh Antre is being thanked here for his help in docking study. The authors are thankful to the Head, Department of Chemistry, Vinyakrao Patil Mahavidyala Vaijapur-423 701 (M.S.), India for partial support of this study. Government Medical College, Aurangabad for providing the experimental animals and Department of Analytical Chemistry, University of Pune; and SAIF, Chandigarh University, Chandigarh, India are thanked for providing spectra of compounds.
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Thore, S.N., Gupta, S.V. & Baheti, K.G. Docking, synthesis, and pharmacological investigation of novel substituted thiazole derivatives as non-carboxylic, anti-inflammatory, and analgesic agents. Med Chem Res 22, 3802–3811 (2013). https://doi.org/10.1007/s00044-012-0382-6
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DOI: https://doi.org/10.1007/s00044-012-0382-6