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新型一氧化氮供体/查耳酮杂合化合物的合成、抗炎活性和致溃疡作用。

Synthesis, anti-inflammatory activity and ulcerogenic liability of novel nitric oxide donating/chalcone hybrids.

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt.

出版信息

Bioorg Med Chem. 2012 Jan 1;20(1):195-206. doi: 10.1016/j.bmc.2011.11.012. Epub 2011 Nov 13.

Abstract

A group of novel nitric oxide (NO) donating chalcone derivatives was prepared by binding various amino chalcones with different NO donating moieties including; nitrate ester, oximes and furoxans. Most of the prepared compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared with indomethacin. The prepared compounds exhibited more protection than indomethacin in regard to gastric toxicity. Histopathological investigation confirmed the beneficial effects of the NO releasing compounds in reducing ulcer formation. The incorporation of the NO-donating group into the parent chalcone derivatives caused a moderate increase in the anti-inflammatory activity with a marked decrease in gastric ulcerations compared to their parent chalcone derivatives.

摘要

一组新型的一氧化氮(NO)供体型查耳酮衍生物通过将各种氨基查尔酮与不同的 NO 供体部分(包括硝酸酯、肟和呋咱)结合而制备。使用角叉菜胶诱导的大鼠足肿胀法,与吲哚美辛相比,大多数制备的化合物表现出显著的抗炎活性。与吲哚美辛相比,这些化合物在胃毒性方面表现出更好的保护作用。组织病理学研究证实了释放 NO 的化合物在减少溃疡形成方面的有益作用。与母体查尔酮衍生物相比,将 NO 供体基团引入母体查尔酮衍生物中会导致抗炎活性适度增加,同时胃溃疡明显减少。

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