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.
MeSH terms
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4-Aminopyridine / analogs & derivatives*
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4-Aminopyridine / chemical synthesis
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4-Aminopyridine / chemistry
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Aminopyridines / chemical synthesis*
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Aminopyridines / chemistry
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Animals
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CHO Cells
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Cell Line
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Cricetinae
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Cricetulus
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Humans
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Positron-Emission Tomography*
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Receptors, Neuropeptide Y / metabolism*
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
Substances
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Aminopyridines
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Receptors, Neuropeptide Y
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Recombinant Proteins
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Thiazoles
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neuropeptide Y-Y1 receptor
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2,4-diaminopyridine
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4-Aminopyridine