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作为镇痛药的苯并咪唑衍生物类曼尼希碱的设计与合成

Design and Synthesis of Mannich bases as Benzimidazole Derivatives as Analgesic Agents.

作者信息

Datar Prasanna A, Limaye Saleel A

机构信息

Department of Pharmaceutical Chemistry, Sinhgad Institute of Pharmacy, Narhe, Pune - 411041, Maharashtra, India.

出版信息

Antiinflamm Antiallergy Agents Med Chem. 2015;14(1):35-46. doi: 10.2174/1871523014666150312164625.

Abstract

Mannich bases were selected for 2D QSAR study to derive meaningful relationship between the structural features and analgesic activity. Using the knowledge of important features a novel series was designed to obtain improved analgesic activity. A series of novel Mannich bases 1-(N-substituted amino)methyl]-2-substituted benzimidazole derivatives were synthesized and were screened for analgesic activity. Some of these compounds showed promising analgesic activity when compared with the standard drug diclofenac sodium.

摘要

选择曼尼希碱进行二维定量构效关系(2D QSAR)研究,以推导结构特征与镇痛活性之间的有意义关系。利用重要特征的知识设计了一个新系列,以获得更好的镇痛活性。合成了一系列新型曼尼希碱1-(N-取代氨基)甲基]-2-取代苯并咪唑衍生物,并对其进行了镇痛活性筛选。与标准药物双氯芬酸钠相比,其中一些化合物显示出有前景的镇痛活性。

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