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新型一氧化氮供体型 1,2,4-三唑/肟类杂合体的合成、抗炎、致溃疡活性和抗增殖活性研究。

New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities.

机构信息

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

出版信息

Bioorg Med Chem. 2013 Jul 1;21(13):3839-49. doi: 10.1016/j.bmc.2013.04.022. Epub 2013 Apr 18.

Abstract

A series of novel nitric oxide (NO) donating triazole/oxime hybrids was prepared and evaluated for their anti-inflammatory activity. Most of the tested compounds showed significant anti-inflammatory activity using carrageenan-induced rat paw edema method compared to indomethacin. Calculation of the ulcer indices and histopathological investigation indicated that the prepared NO-donating oximes exhibited less ulcerogenicity compared to their intermediate ketones and indomethacin. The NO-donating oxime 6i revealed significant activity against renal cancer A498 cell lines with 50.52 cell growth inhibition.

摘要

一系列新型的含一氧化氮(NO)供体三唑/肟类化合物被合成并评估其抗炎活性。与吲哚美辛相比,用角叉菜胶诱导的大鼠足肿胀法测定,大多数测试化合物表现出显著的抗炎活性。计算溃疡指数和组织病理学研究表明,与中间酮和吲哚美辛相比,所制备的含 NO 供体肟类化合物的致溃疡作用较小。NO 供体肟 6i 对肾癌细胞 A498 细胞系具有显著的活性,细胞生长抑制率为 50.52%。

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