Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives

European Journal of Medicinal Chemistry
Mai E ShomanMohamed A Morsy

Abstract

A group of 3,5-diaryl-2-pyrazoline derivatives were prepared via the reaction of various chalcones with hydrazine hydrate in ethanol. A group of NO-donating-2-pyrazoline derivatives were synthesized by carrying a nitrate ester group or an oxime group onto the prepared pyrazoline derivatives through different spacers. The prepared compounds were evaluated for their anti-inflammatory activity using carrageenan-induced rat paw edema and compared to a well-known NSAID, indomethacin as a reference drug. The ability of the prepared compounds to induce gastric toxicity was also evaluated. Most of the prepared compounds showed significant anti-inflammatory activity at the injected dose (100mg/kg) but they were safer than indomethacin in regard to gastric toxicity. The incorporation of the NO-donating group into the parent pyrazoline derivatives caused a non-significant reduction in the anti-inflammatory activity while a marked decrease in gastric ulcerations induced by their parent pyrazolines was observed.

Citations

Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Xue-Qun Fu
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Xue BaiShu-Fan Yin
Dec 27, 2011·Acta Crystallographica. Section E, Structure Reports Online·Phonpawee NonthasonHoong-Kun Fun
Feb 22, 2012·Acta Crystallographica. Section E, Structure Reports Online·Hoong-Kun FunSuchada Chantrapromma
Jul 17, 2012·Acta Crystallographica. Section E, Structure Reports Online·Hoong-Kun FunThawanrat Kobkeatthawin
Jul 10, 2010·International Journal of Medical Sciences·Ibrahim A AlsarraSteven H Neau
Aug 11, 2012·European Journal of Medicinal Chemistry·Adithya AdhikariRavish Sankolli
Oct 27, 2011·Pharmaceuticals·Priscila Longhin BosquesiMan Chin Chung
Mar 2, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Seham Y Hassan
Jan 14, 2011·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Abdullah M Asiri, Salman A Khan
Oct 11, 2013·Acta Crystallographica. Section E, Structure Reports Online·Thitipone SuwunwongHoong-Kun Fun
Sep 23, 2020·Archiv der Pharmazie·Hossameldin A AzizSamar H Abbas
Mar 9, 2012·Expert Opinion on Therapeutic Patents·Mohamed R ShaabanAhmad M Farag
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Martha MantzanidouDimitra Hadjipavlou-Litina
Aug 23, 2019·Organic Letters·Samuel ThurowIgor D Jurberg

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