| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365854 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
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.
Graphical abstractThe 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 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide
