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首页> 美国卫生研究院文献>Journal of Chemical Biology >Synthesis of tert-butyl (substituted benzamido)phenylcarbamate derivatives: anti-inflammatory activity and docking studies
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Synthesis of tert-butyl (substituted benzamido)phenylcarbamate derivatives: anti-inflammatory activity and docking studies

机译：叔丁基（取代的苯甲酰胺基）苯基氨基甲酸酯衍生物的合成：抗炎活性和对接研究

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A series of new tert-butyl 2-(substituted benzamido) phenylcarbamate >(4a–>4j) were synthesized by the condensation of tert-butyl 2-amino phenylcarbamate (>3) with various substituted carboxylic acid in the presence of EDCI and HOBt as coupling reagent, obtain in excellent yields. The structures of all newly synthesized compounds were characterized spectroscopically and evaluated for in vivo anti-inflammatory activity compared to the standard drug, indomethacin, by using the carrageenan-induced rat paw edema protocol. Most of the compounds exhibited a promising anti-inflammatory activity within 9 to 12 h, the percentage of inhibition values ranging from 54.239 to 39.021%. The results revealed that the compounds >4i and >4a exhibited better or equivalent anti-inflammatory activity with the percentage of inhibition of 54.239 and 54.130%, respectively, which was comparable to standard drug. In addition to experimental results, in silico docking studies was used as a tool to verify and expand the experimental outcomes.Electronic supplementary materialThe online version of this article (doi:10.1007/s12154-017-0168-x) contains supplementary material, which is available to authorized users.
机译：通过2-氨基苯基氨基甲酸叔丁酯缩合反应合成了一系列新的2-（取代的苯甲酰胺）苯基氨基甲酸叔丁酯>（4a – > 4j）。 3 ），在EDCI和HOBt的存在下，用各种取代的羧酸作为偶联剂，可获得极好的收率。使用角叉菜胶诱导的大鼠爪水肿方案，与标准药物吲哚美辛相比，对所有新合成化合物的结构进行光谱表征，并评估其体内抗炎活性。大多数化合物在9到12小时内显示出有希望的抗炎活性，抑制值的百分比范围为54.239至39.021％。结果表明，化合物> 4i 和> 4a 表现出更好或相当的抗炎活性，抑制百分比分别为54.239％和54.130％，与标准药物相当。除实验结果外，计算机对接研究还用作验证和扩展实验结果的工具。电子补充材料本文的在线版本（doi：10.1007 / s12154-017-0168-x）包含补充材料，该材料是可供授权用户使用。

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