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1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists

Mills, Sander G ; Wu, Mu Tsu ; Maccoss, Malcolm ; Budhu, Richard J ; Dorn, Conrad P ; Cascieri, Margaret A ; Sadowski, Sharon ; Strader, Catherine D ; Greenlee, William J

Bioorganic & Medicinal Chemistry Letters, 1993, Vol.3(12), pp.2707-2712 [Peer Reviewed Journal]

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  • Title:
    1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists
  • Author: Mills, Sander G ; Wu, Mu Tsu ; Maccoss, Malcolm ; Budhu, Richard J ; Dorn, Conrad P ; Cascieri, Margaret A ; Sadowski, Sharon ; Strader, Catherine D ; Greenlee, William J
  • Description: A series of N,N′-diacylpiperazine-2-carboxamides are shown to be antagonists of the NK-1 (Substance P) receptor. Elaboration of the C2 sidechain with aminoalkyl groups leads to two series of potent antagonists, one containing simple dialkylamino groups and the second featuring 2-methoxybenzylamino derivatives with divergent SARs with respect to substitution at the C2 amide bond. A series of N,N′-diacylpiperazine-2-carboxamides are shown to be potent, selective antagonists of the NK-1 (Substance P) receptor.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 1993, Vol.3(12), pp.2707-2712
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/S0960-894X(01)80747-2
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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