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某些1,2,4-三嗪衍生物的合成及其镇痛抗炎活性

Synthesis and analgesic-anti-inflammatory activities of some 1,2,4-triazine derivatives.

作者信息

Makhlouf Abdelmoneim A, Maklad Yousreya A

机构信息

Chemistry Department, Faculty of Science, Cairo University (Fayoum Branch), Fayoum, Egypt.

出版信息

Arzneimittelforschung. 2004;54(1):42-9. doi: 10.1055/s-0031-1296935.

DOI:10.1055/s-0031-1296935
PMID:14979608
Abstract

A variety of novel N-arylidene-N'-[5-(4-isobutylphenyl)-[1,2,4]-triazin-3-yl] hydrazines 4, carboxylic acid N'-[5-(4-isobutylphenyl)-[1,2,4]-triazin-3-yl] hydrazides 5, triazolotriazines 6 and other related triazine derivatives were synthesized. Several synthetic routes were employed to access the desired compounds from 5-(4-isobutylphenyl)-[1,2,4]-triazin-3-yl hydrazine 3 as a parent compound. The analgesic and anti-inflammatory activities of the synthesized compounds were studied. The results showed that compound 4 g exhibited pronounced analgesic activity, while compound 4f displayed the highest anti-inflammatory activity. Meanwhile, compound 6d evoked dual analgesic-anti-inflammatory effect without any ulcerogenicity.

摘要

合成了多种新型的N-亚芳基-N'-[5-(4-异丁基苯基)-[1,2,4]-三嗪-3-基]肼4、羧酸N'-[5-(4-异丁基苯基)-[1,2,4]-三嗪-3-基]酰肼5、三唑并三嗪6以及其他相关的三嗪衍生物。采用了几种合成路线,以5-(4-异丁基苯基)-[1,2,4]-三嗪-3-基肼3作为母体化合物来制备所需化合物。研究了合成化合物的镇痛和抗炎活性。结果表明,化合物4g表现出显著的镇痛活性,而化合物4f显示出最高的抗炎活性。同时,化合物6d引起了双重镇痛-抗炎作用,且无任何致溃疡作用。

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