SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF N-METHYL PIPERIDINE ANALGESICS

Abstract

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, the N-methyl piperidine molecule was derivatized with various phenacyl halides and the resultant quaternary derivatives were explored extensively for analgesic activity using the tail flick test. Spectrophotometric techniques such as UV, IR, Proton NMR and Mass (EI) were also utilized to confirm the structures of the newly-synthesized compounds. All the compounds exhibited analgesic activity and particularly 1-[3', 4'-dihydroxyphenacyl) - N - methylpiperidinium bromide showed approximately one twentieth the analgesic activity of morphine