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1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists

Mills, Sander G ; Maccoss, Malcolm ; Underwood, Dennis ; Shah, Shrenik K ; Finke, Paul E ; Miller, Daniel J ; Budhu, Richard J ; Cascieri, Margaret A ; Sadowski, Sharon ; Strader, Catherine D

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(13), pp.1345-1350 [Peer Reviewed Journal]

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  • Title:
    1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists
  • Author: Mills, Sander G ; Maccoss, Malcolm ; Underwood, Dennis ; Shah, Shrenik K ; Finke, Paul E ; Miller, Daniel J ; Budhu, Richard J ; Cascieri, Margaret A ; Sadowski, Sharon ; Strader, Catherine D
  • Description: A stereocontrolled synthesis of 1-benzyloxy-2-phenylcyclohexane derivatives containing polar substituents at C3 is described. These compounds, designed to test the role of the ring nitrogen in a related series of potent piperidine-based substance P antagonists, show similar NK-1 receptor affinity, indicating that the nitrogen may serve a largely structural role in N-substituted piperidine antagonists. Replacing the ring nitrogen of L-736,281 (X = N) with carbon provides an NK-1 antagonist of identical potency, indicating that in N-substituted piperidine antagonists, the nitrogen may serve largely as a scaffold for the presentation of other pharmacophores.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(13), pp.1345-1350
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/0960-894X(95)00220-N
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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