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

…, M Ando, C Nakama, K Kobayashi, H Kawamoto…

Index: Kameda, Minoru; Ando, Makoto; Nakama, Chisato; Kobayashi, Kensuke; Kawamoto, Hiroshi; Ito, Sayaka; Suzuki, Tomoki; Tani, Takeshi; Ozaki, Satoshi; Tokita, Shigeru; Sato, Nagaaki Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 17 p. 5124 - 5127

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Citation Number: 9

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.

Bioisosteric replacements of the pyrazole moiety of rimonaba...

[Lange, Jos H. M.; Van Stuivenberg, Herman H.; Coolen, Hein K. A. C.; Adolfs, Tiny J. P.; McCreary, Andrew C.; Keizer, Hiskias G.; Wals, Henri C.; Veerman, Willem; Borst, Alice J. M.; De Looff, Wouter; Verveer, Peter C.; Kruse, Chris G. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1823 - 1838]