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Issue 7, 2014
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Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor

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Abstract

A series of triazospirodecanone derivatives were synthesized as potential NOP ligands. 8-(Chroman-4-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (4) and its 5-fluoro analogue (18) proved to be active as agonists with EC50 values in the submicromolar range. Single enantiomers of compound 4 were separated and tested as NOP agonists; the eutomer R-(+)-4 showed a pEC50 of 7.34. Finally docking studies were performed on the NOP receptor to identify the most significant stereospecific interactions.

Graphical abstract: Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor

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Publication details

The article was received on 24 Feb 2014, accepted on 22 Apr 2014 and first published on 23 Apr 2014


Article type: Concise Article
DOI: 10.1039/C4MD00082J
Citation: Med. Chem. Commun., 2014,5, 973-983
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    Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor

    U. M. Battisti, S. Corrado, C. Sorbi, A. Cornia, A. Tait, D. Malfacini, M. C. Cerlesi, G. Calò and L. Brasili, Med. Chem. Commun., 2014, 5, 973
    DOI: 10.1039/C4MD00082J

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