1044269-84-2Relevant academic research and scientific papers
Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists
Leslie, Colin P.,Bentley, Jonathan,Biagetti, Matteo,Contini, Stefania,Di Fabio, Romano,Donati, Daniele,Genski, Thorsten,Guery, Sebastien,Mazzali, Angelica,Merlo, Giancarlo,Pizzi, Domenica A.,Sacco, Fabiola,Seri, Catia,Tessari, Michela,Zonzini, Laura,Caberlotto, Laura
scheme or table, p. 6103 - 6107 (2010/12/18)
A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5]decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine sub-nanomolar Y5 activity with metabolic stability, oral bioavailability, brain penetration and strong preclinical profile for development. Both compounds significantly inhibited the food intake induced by a Y5 selective agonist with minimal effective doses of 3 mg/kg po.
