Synthesis and analgesic potential of 4-[4–chloro-3- (trifluoromethyl)-phenyl]-4-piperidinol analogues against pain model in mice

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, 1 H-NMR, 13 C-NMR, UV, and FT-IR). The analgesic action of the sy...

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Veröffentlicht in:Medicinal chemistry research 2022-04, Vol.31 (4), p.617-627
Hauptverfasser: Haider, Shazia, Saify, Zafar Saied, Mushtaq, Nousheen, Siddiqui, Faheema, Rao, Toqeer Ahmed, Mallick, Tabinda Zareen, Begum, Nasreen
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Sprache:eng
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Zusammenfassung: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, 1 H-NMR, 13 C-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.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-022-02860-8