Author/Authors :
Jonathan R. Young، نويسنده , , Ronsar Eid، نويسنده , , Cherilyn Turner، نويسنده , , Robert J. DeVita، نويسنده , , Marc M. Kurtz، نويسنده , , Kwei-Lan C. Tsao، نويسنده , , Gary G. Chicchi، نويسنده , , Alan Wheeldon، نويسنده , , Emma Carlson، نويسنده , , Sander G. Mills، نويسنده ,
Abstract :
The preparation and structure–activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK1 antagonists in vitro and efficacious in vivo with minimal interactions with P450 liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.
