Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
作者信息
Kameda Minoru, Ando Makoto, Nakama Chisato, Kobayashi Kensuke, Kawamoto Hiroshi, Ito Sayaka, Suzuki Tomoki, Tani Takeshi, Ozaki Satoshi, Tokita Shigeru, Sato Nagaaki
机构信息
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo 3, Tsukuba, Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5124-7. doi: 10.1016/j.bmcl.2009.07.030. Epub 2009 Jul 10.
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.
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