1630952-69-0Relevant articles and documents
Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor
Battisti, Umberto M.,Corrado, Sandra,Sorbi, Claudia,Cornia, Andrea,Tait, Annalisa,Malfacini, Davide,Cerlesi, Maria Camilla,Calò, Girolamo,Brasili, Livio
, p. 973 - 983 (2014/07/08)
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 pEC 50 of 7.34. Finally docking studies were performed on the NOP receptor to identify the most significant stereospecific interactions.