Synthesis and Binding Affinity of Fluorine Containing NG-acyl and -sulfonyl BIBP3226 Derivatives: Ligands for the NPY Y1 Receptor

2016 
The neuropeptide Y (NPY) receptors are abundant in a range of tumours hence are a molecular target for tumour imaging and therapy, particularly by the use of radiolabelled molecules. NG-Substituted derivatives of the NPY receptor antagonist, BIBP3226, were prepared aiming to improve its current usability and to incorporate a positron-emitting radioisotope for development in positron emission tomography (PET) radiopharmaceuticals. The BIBP3226 derivatives were prepared in seven steps while retaining the critically important amino acid chirality. The acyl derivative retained acceptable ligand binding, however the sulfonyl derivatives lost almost all binding affinity.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    32
    References
    0
    Citations
    NaN
    KQI
    []