Title of article
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5310
To page
5315
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.
Keywords
Substance P , NK1 antagonists
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798603
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