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Pyrrolidine-carboxamides and oxadiazoles as potent hNK 1 antagonists

Young, Jonathan R. ; Eid, Ronsar ; Turner, Cherilyn ; Devita, Robert J. ; Kurtz, Marc M. ; Tsao, Kwei-Lan C. ; Chicchi, Gary G. ; Wheeldon, Alan ; Carlson, Emma ; Mills, Sander G.

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(19), pp.5310-5315 [Peer Reviewed Journal]

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  • Title:
    Pyrrolidine-carboxamides and oxadiazoles as potent hNK 1 antagonists
  • Author: Young, Jonathan R. ; Eid, Ronsar ; Turner, Cherilyn ; Devita, Robert J. ; Kurtz, Marc M. ; Tsao, Kwei-Lan C. ; Chicchi, Gary G. ; Wheeldon, Alan ; Carlson, Emma ; Mills, Sander G.
  • Description: The preparation and structure–activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK 1 antagonists in vitro and efficacious in vivo with minimal interactions with P 450 liver enzymes. Oxadiazole 22 was determined to have excellent hNK 1 binding affinity, functional activity, and a good PD response in vivo. The preparation and structure–activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK 1 antagonists in vitro and efficacious in vivo with minimal interactions with P 450 liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK 1 binding affinity, functional activity, and a good PD response in vivo.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(19), pp.5310-5315
  • Identifier: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2007.08.028
  • Subjects: Nk 1 Antagonists ; Substance P
  • Language: English

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