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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives.
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Synthesis and investigation of anti-inflammatory activity and gastric ulcerogenicity of novel nitric oxide-donating pyrazoline derivatives.

机译：新型提供一氧化氮的吡唑啉衍生物的合成及抗炎活性和胃溃疡的研究。

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摘要

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.
机译：通过各种查耳酮与水合肼在乙醇中的反应制备了一组3,5-二芳基-2-吡唑啉衍生物。通过将硝酸酯基或肟基通过不同的间隔基携带到所制备的吡唑啉衍生物上，来合成一组NO-给体-2-吡唑啉衍生物。使用角叉菜胶诱导的大鼠爪水肿评估所制备的化合物的抗炎活性，并与众所周知的NSAID吲哚美辛作为参考药物进行比较。还评估了制备的化合物诱导胃毒性的能力。大多数制备的化合物在注射剂量（100mg / kg）下均表现出显着的抗炎活性，但就胃毒性而言，它们比消炎痛更安全。将NO-给体基团掺入母体吡唑啉衍生物中引起抗炎活性无明显降低，同时观察到其母体吡唑啉诱导的胃溃疡明显减少。

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