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
{"title":"Synthesis, Pharmacological Evaluation and In-Silico Studies of Some Piperidine Derivatives as Potent Analgesic Agents","authors":"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","doi":"10.4172/2329-6631.1000170","DOIUrl":null,"url":null,"abstract":"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. \nGraphical abstract","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"1 1","pages":"1-9"},"PeriodicalIF":0.0000,"publicationDate":"2017-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Developing Drugs","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4172/2329-6631.1000170","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 3
Abstract
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