• Title of article

    Synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere and its use in the development of melanocortin receptor agonists

  • Author/Authors

    Xinrong Tian، نويسنده , , Xuemei Chen، نويسنده , , Lixian Gan، نويسنده , , Jeffery C. Hayes، نويسنده , , Adrian G. Switzer، نويسنده , , Mark G. Solinsky، نويسنده , , Frank H. Ebetino، نويسنده , , John A. Wos، نويسنده , , Beth B. Pinney، نويسنده , , Julie A. Farmer، نويسنده , , Doreen Crossdoersen، نويسنده , , Russell J. Sheldon، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2006
  • Pages
    5
  • From page
    1721
  • To page
    1725
  • Abstract
    The first synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere is described, which features diastereoselective alkylation of the tricyclic lactam 14. The use of this novel dipeptide isostere in the development of melanocortin agonists has been demonstrated by the synthesis of peptidomimetic 7 and non-peptidic ligand 27. Both compounds displayed significant binding and agonist potency at the MC4R.
  • Keywords
    Melanocortin agonists
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2006
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    796652