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Synthesis and anti-inflammatory activity of some pyrazole derivatives

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Abstract

A novel series of pyrazoles containing benzenesulfonamides, 1,3,4-oxadiazole-2-thiones, 4-substituted-1,2,4-triazole-3-thiones, and 2-substituted-1,3,4-thiadiazoles has been synthesized. Anti-inflammatory activity of some synthesized compounds was evaluated in vivo utilizing a standard acute carrageenan-induced paw edema method. The most active anti-inflammatory agents 3, 8f, and 10f were evaluated for ulcerogenic liability in rats compared to indomethacin and celecoxib as reference standards. Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior.

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Acknowledgments

The authors thank Dr. Ehab T. Abdel-Raheem (Department of Pharmacology, Faculty of Pharmacy, Assiut University, Assiut, Egypt) for his kind interest, valuable discussions during pharmacological screening.

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Correspondence to Hamdy M. Abdel-Rahman.

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El-Moghazy, S.M., Barsoum, F.F., Abdel-Rahman, H.M. et al. Synthesis and anti-inflammatory activity of some pyrazole derivatives. Med Chem Res 21, 1722–1733 (2012). https://doi.org/10.1007/s00044-011-9691-4

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