哌啶类强效镇痛药物的合成、药理评价及计算机研究

Journal of Developing Drugs Pub Date : 2017-03-24 DOI:10.4172/2329-6631.1000170

S. Ansari, Sadia Arif, N. Mushtaq, Ahsaan Ahmed, S. Akhtar, Rabya Munawar, H. Naseem, S. Meer, Z. S. Saify, M. Arif, Qurrat-ul-ain Leghari

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引用次数: 3

摘要

本研究合成了一些4-哌啶哌替啶(PP)和4-氨基甲基哌啶(AMP)衍生物PP1-3和AMP4-9，以探索它们的镇痛潜力。体内热(尾浸)法评价化合物活性，不同剂量下均产生显著的镇痛作用。对接结果说明合成的衍生物具有良好的结合亲和力，所有化合物都可能与mu-阿片受体相互作用。与标准化合物(芬太尼、吗啡、哌替啶)相比，合成化合物的药效模型显示出可能具有镇痛活性所需的结构特征。在所有的PP1中，AMP5和AMP6是有效的镇痛剂。图形抽象

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Synthesis, Pharmacological Evaluation and In-Silico Studies of Some Piperidine Derivatives as Potent Analgesic Agents

In present study, some 4-piperidinopiperidine (PP) and 4-amino methylpiperidine (AMP) derivatives (PP1-3 and AMP4-9) have been synthesized to explore their analgesic potential. Activity of compounds evaluated by in-vivo thermal (tail immersion) method produced significant analgesia at different doses. Docking results explained good binding affinity of synthesized derivatives and potential interaction of all compounds with mu-opioid receptor. The pharmacophoric model of synthesized compounds showed possible structural features required for analgesic activity when compared with standards (Fentanyl, Morphine, Pethidine). Among all PP1, AMP5 and AMP6 emerged out as potent analgesic agents. Graphical abstract

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Journal of Developing Drugs

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