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抗氧化型吲哚美辛衍生物的合成及其活性研究
引用本文:张一纯,陈平涛,管华诗,李英霞.抗氧化型吲哚美辛衍生物的合成及其活性研究[J].中国化学,2005,23(11):1523-1529.
作者姓名:张一纯  陈平涛  管华诗  李英霞
作者单位:Key Laboratory of Marine Drugs, The Ministry of Education of China, Marine Drug and Food Institute, Ocean University of China, Qingdao, Shandong 266003, China
基金项目:Project supported by the Young Scientist Foundation of Shandong Province (No. 03BS047).
摘    要:将NSAID吲哚美辛与七种天然酚类抗氧化剂偶连,合成了一系列具有抗氧化活性的吲哚美辛衍生物,试图发挥抗炎和抗氧化的双重功效,以降低吲哚美辛的胃肠毒性,同时提高其抗炎活性。对14个目标产物的抗氧化活性和抗炎活性进行了研究,发现上述化合物均表现出明显的抗氧化能力,但没有表现出明显的抑制巴豆油导致的小鼠耳肿胀作用。

关 键 词:消炎痛  抗氧化剂  药物  药理作用  合成方法
收稿时间:2005-02-18
修稿时间:2005-02-182005-07-18

Synthesis and Pharmacological Evaluation of Novel Conjugates of Indomethacin with Antioxidant Activity
ZHANG,;Yi-Chun;CHEN,;Ping-Tao;GUAN,;Hua-Shi;LI,;Ying-Xia.Synthesis and Pharmacological Evaluation of Novel Conjugates of Indomethacin with Antioxidant Activity[J].Chinese Journal of Chemistry,2005,23(11):1523-1529.
Authors:ZHANG  ;Yi-Chun;CHEN  ;Ping-Tao;GUAN  ;Hua-Shi;LI  ;Ying-Xia
Abstract:A series of new conjugates of indomethacin with phenolic anfioxidants were synthesized for enhanced antiinflammatory activity as well as reduced ulcerogenic potency. It was found that all conjugates were very potent antioxidants in vitro. They could inhibit lipid peroxidafion significantly, while 11b-11e and 13b-13e could also interact with DPPH. However these conjugates showed little inhibition against croton oil induced mouse ear swelling.
Keywords:antioxidant  indomethacin  antiinflammation  conjugate  nonsteroidal antiinflammatory drugs (NSAID)
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