113771-46-3Relevant 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.
Compounds that modulate PPAR activity and methods of preparation
-
, (2008/06/13)
This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.
Hydrogenated 1-benzooxacycloalkylpyridinecarboxylic acid compounds
-
, (2008/06/13)
The invention relates to novel hydrogenated 1-benzooxacycloalkylpyridinecarboxylic acid compounds of formula STR1 in which the variable R1, R2, R3, R4, R5, alk, X, Z, m, n and p, the dotted line and t
