敖桂珍, 张奕华, 季晖, 邓钢. α-取代的对甲磺酰基苯丙烯酰胺的合成及抗炎活性J. 药学学报, 2003, 38(9): 671-676.
引用本文: 敖桂珍, 张奕华, 季晖, 邓钢. α-取代的对甲磺酰基苯丙烯酰胺的合成及抗炎活性J. 药学学报, 2003, 38(9): 671-676.
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AO Gui-zhen, ZHANG Yi-hua, JI Hui, DENG Gang. Synthesis and anti-inflammatory activity of α-substituted P-(methanesulfonyl)phenylpropenamidesJ. Acta Pharmaceutica Sinica, 2003, 38(9): 671-676.
Citation: AO Gui-zhen, ZHANG Yi-hua, JI Hui, DENG Gang. Synthesis and anti-inflammatory activity of α-substituted P-(methanesulfonyl)phenylpropenamidesJ. Acta Pharmaceutica Sinica, 2003, 38(9): 671-676.
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α-取代的对甲磺酰基苯丙烯酰胺的合成及抗炎活性

Synthesis and anti-inflammatory activity of α-substituted P-(methanesulfonyl)phenylpropenamides

    摘要
  • 摘要: 目的寻找高效低毒的非甾体抗炎药。方法合成α-取代的对甲磺酰基苯丙烯酰胺，评价其抗炎活性，并考察连续经口给药对大鼠胃肠道（GI）的影响。结果合成了25个新化合物（II1-25），其结构经IR、1H NMR、MS和元素分析确证。角叉菜胶致大鼠足跖肿胀模型试验结果显示，12个化合物(II1,3,5,7,8,10-12,17,18,20,23)的抗炎活性与双氯芬酸钠（DC）和罗非昔布（RC）相当（P>0.05）。其中II3,8,10,11,18,20的GI副作用均显著小于DC(P<0.01)，与RC和羧甲基纤继素钠(CMC-Na)无明显差别(P>0.05)。结论α-取代的对甲磺酰基苯丙烯酰胺抗炎活性强，GI不良反应低，值得深入研究。

     

    Abstract: AimTo search for new compounds with strong anti-inflammatory activity and low gastrointestinal (GI) side effects. MethodsA series of α-substituted P-(methanesulfonyl)phenyl-propenamides were synthesized. Their anti-inflammatory activities against xylene-induced mice ear swelling and carrageenan-induced rat paw edema were evaluated, and their GI side effects in rats were examined. ResultsTwenty-five target compounds (II1-25) were obtained, and their structures were determined by IR, 1H NMR, MS and elemental analysis. Thirteen compounds (II1,3,5,8-13,15,18,19,23) exhibited marked anti-inflammatory activity comparable to diclofenac sodium (DC) and rofecoxib (RC) in xylene-induced mice ear swelling model, and twelve compounds (II1,3,5,7,8,10-12,17,18,20,23) showed remarkable anti-inflammatory activity comparable to DC and RC in carrageenan-induced rat paw edema. Compounds II3,8,10,11,18,20 showed GI side effects less than DC (P<0.01), and no significant difference compared with RC and CMC-Na (P>0.05). Conclusionα-Substituted P-(methanesulfonyl)phenylpropenamides showed strong anti-inflammatory activity but few GI side effects and deserve to be further investigated.

     

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