医薬品開発ジャーナル
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概要

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

Sumaira Ansari, Sadia Arif, Nousheen Mushtaq, Ahsaan Ahmed, Shamim Akhtar , Rabya Munawar, Huma Naseem, Sadia Meer, Zafar Saied Saify, Muhammad Arif and Qurratul-ain Leghari

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