Abstract
In the study of designing pharmacophore models for analgesic, a series of 4-[4–chloro-3- (trifluoromethyl)-phenyl]-4-piperidinol (TFMP) derivatives were synthesized and characterized by physical and spectral method (HR-EIMS, HR-FABMS, 1H-NMR, 13C-NMR, UV, and FT-IR). The analgesic action of the synthesized derivatives was estimated by means of Hot Plate Method. Most of the compounds displayed potent analgesic efficacy and an ultrashort to long duration of action. The results indicate that these compounds are useful as analgesics. In the presence of naloxone they displayed pain reliving effect. In conclusion, among active compounds 3 (188%), 5 (137%), 6 (162%), and 8 (107%) respectively, emerged as most effective analgesic and they depressed peripheral and centrally mediated pain by opioid independent systems.
Highlights
Pain is a complex body response to noxious stimulus both chemical or physical or chemical [1, 2]
We report here the synthesis of 4-[4–chloro-3--phenyl]-4-piperidinol (TFMP) derivatives 1–12 via the reactions of TFMP by nucleophilic substitution with a variety of alkylating agent by N-alkylation
Structure-activity relationship (SAR) study specified that the activity of these 4-[4–chloro-3--phenyl]-4piperidinol (TFMP) derivatives could be due to different acetophenone substituents
Summary
Pain is a complex body response to noxious stimulus both chemical (acetic acid and formalin) or physical (heat and cold pressure,) or chemical (acetic acid and formalin) [1, 2]. Variety of prescribed medicines are existing for managing of pain, opioid drugs, exclusively those substituted μ-opioid receptor and associated ways. They have established to be the utmost active, regardless of more or less severe side effects comprising addiction, dependence, respiratory depression, pruritus, nausea, hypotension, and constipation. Valuation of novel chemical compounds as analgesic agents by using animal models is a complex assignment. Researchers have developed a relationship between animal models and human clinical responses. These methods are simple, reproducible and sensitive to discover weak and potent analgesic agents. The compounds being synthesized will be added to the current information of piperidine substituted compounds in the development of drugs
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
