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新型杂芳基羧酸衍生物作为抗炎镇痛药的合成及生物学评价

Synthesis and biological evaluation of new heteroaryl carboxylic acid derivatives as anti-inflammatory-analgesic agents.

作者信息

Abouzid Khaled Abouzid Mohamed, Khalil Nadia Abdalla, Ahmed Eman Mohamed, Zaitone Sawsan Abo-Bakr

机构信息

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt.

出版信息

Chem Pharm Bull (Tokyo). 2013;61(2):222-8. doi: 10.1248/cpb.c12-00949.

Abstract

A series of nicotinic acid derivatives structurally related to niflumic acid and certain pyridazine-containing compounds have been synthesized and characterized by analytical and spectral data. All compounds were screened for their potential analgesic and anti-inflammatory activities. The compounds which displayed analgesic and anti-inflammatory activities were tested for ulcerogenicity and screened for in vivo inhibition of certain inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and cyclooxygenase-2 (COX-2). Compounds 1c, 2a, 2b, and 5a have shown potent analgesic and anti-inflammatory activities.

摘要

已经合成了一系列在结构上与尼氟酸相关的烟酸衍生物以及某些含哒嗪的化合物,并通过分析和光谱数据对其进行了表征。对所有化合物的潜在镇痛和抗炎活性进行了筛选。对显示出镇痛和抗炎活性的化合物进行了致溃疡作用测试,并筛选了其对某些炎性细胞因子如肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)和环氧合酶-2(COX-2)的体内抑制作用。化合物1c、2a、2b和5a已显示出强效的镇痛和抗炎活性。

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