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  • Title: Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
    Author: Young JR, Eid R, Turner C, DeVita RJ, Kurtz MM, Tsao KL, Chicchi GG, Wheeldon A, Carlson E, Mills SG.
    Journal: Bioorg Med Chem Lett; 2007 Oct 01; 17(19):5310-5. PubMed ID: 17723300.
    Abstract:
    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.
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