Synthesis, Pharmacological Evaluation and In-Silico Studies of Some Piperidine Derivatives as Potent Analgesic Agents
نویسندگان
چکیده
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.
منابع مشابه
SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF N-METHYL PIPERIDINE ANALGESICS
Pain is probably the immediate stimulus for more visits to the Physician's office than all other complaints combined. Since pain serves as an alert to injury, it is often the first harbinger of disease. Piperidine has been extensively utilized for the synthesis of a wide range of therapeutic agents in general and analgetics in particular for the mitigation of pain. In a similar attempt, th...
متن کاملSynthesis of Some Benzofuran Derivatives Containing Pyrimidine Moiety as Potent Antimicrobial Agents
In this investigation, the synthesis of 2-substituted pyrimidines by the reaction of benzofuranchalcones (3a-d) with urea, thiourea and guanidine hydrochloride was reported. The structuresof title compounds (4a-d), (5a-d) and (6a-d) were established on the basis of analyticaland spectral data. The synthesized compounds were screened for antimicrobial activityand molecular docking studies. Some ...
متن کاملSynthesis,Characterization, Biological Evaluation and anti corrosion activity of some new bis-piperidone Derivatives
Aseries of piperidine derivatives was synthesis by the reaction between substituted benzaldhyde ,pentanone-3,and ammonium acetate by refluxining for 1-2 hr in ethanol and the derivatives refluxed with (4,4'-Diaminodiphenyl sulphone) yielded bispiperidine ,the structures of the synthesized compounds were confirmed by spectroscopy analysis , The reported compounds were screened for their antibact...
متن کاملSynthesis of Some Benzofuran Derivatives Containing Pyrimidine Moiety as Potent Antimicrobial Agents
In this investigation, the synthesis of 2-substituted pyrimidines by the reaction of benzofuranchalcones (3a-d) with urea, thiourea and guanidine hydrochloride was reported. The structuresof title compounds (4a-d), (5a-d) and (6a-d) were established on the basis of analyticaland spectral data. The synthesized compounds were screened for antimicrobial activityand molecular docking studies. Some ...
متن کاملSynthesis,Characterization, Biological Evaluation and anti corrosion activity of some new bis-piperidone Derivatives
Aseries of piperidine derivatives was synthesis by the reaction between substituted benzaldhyde ,pentanone-3,and ammonium acetate by refluxining for 1-2 hr in ethanol and the derivatives refluxed with (4,4'-Diaminodiphenyl sulphone) yielded bispiperidine ,the structures of the synthesized compounds were confirmed by spectroscopy analysis , The reported compounds were screened for their antibact...
متن کامل