62620-31-9Relevant academic research and scientific papers
Synthesis and Structure-Activity Relationships of Triazaspirodecanone Derivatives as Nociceptin/Orphanin FQ Receptor Ligands
Corrado, Sandra,Battisti, Umberto M.,Sorbi, Claudia,Tait, Annalisa,Malfacini, Davide,Camarda, Valeria,Calò, Girolamo,Brasili, Livio
, p. 447 - 458 (2015/02/19)
Several spiroxatrine derivatives were synthesized and evaluated as potential NOP receptor ligands. Structural modifications of the 1,4-benzodioxane moiety of spiroxatrine have been the focus of this research project. The structure-activity relationships that emerged indicate that the presence of an H-bond donor group (hydroxyl group) is more favorable for NOP activity when it is positioned α with respect to the CH2 linked to the 1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one portion. Moreover, cis diastereoisomers of the hydroxyl derivatives4 and 22 show a moderately higher degree of stereoselectivity than trans isomers. In particular, the spiropiperidine derivative cis-4 has submicromolar agonistic activity, and it will be the reference compound for the design and synthesis of new NOP agonists.
1,3,8-Triazaspiro(4.5)decan-4-one derivatives
-
, (2008/06/13)
Compounds having the structure STR1 and the pharmaceutically acceptable salts thereof, wherein R1 is hydrogen, halogen, hydroxy, alkanoyloxy, alkoxy, alkylthio, alkyl or trifluoromethyl; R2 is hydrogen, alkyl or alkenyl; R3 is hydrogen, halogen or alkyl; R4 is formyloxy or alkanoyloxy; m is 1 or 2; and n is 0, 1 or 2; have useful physiological activity.
