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Bioorg Med Chem Lett. 2009 Sep 1;19(17):5124-7. doi: 10.1016/j.bmcl.2009.07.030. Epub 2009 Jul 10.

Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.

Author information

1
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo 3, Tsukuba, Ibaraki, Japan.

Abstract

A series of 2,4-diaminopyridine derivatives was synthesized and evaluated as potential candidates for neuropeptide Y (NPY) Y1 receptor positron emission tomography (PET) tracers. Derivatives bearing substitutions allowing reliable access to radiolabeling were designed, focusing on Y1 binding affinity and lipophilicity. The advanced derivatives 2n and 2o were identified as promising PET tracer candidates.

PMID:
19640706
DOI:
10.1016/j.bmcl.2009.07.030
[Indexed for MEDLINE]

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