Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors.
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.
Kameda
Minoru
M
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo 3, Tsukuba, Ibaraki, Japan.
Ando
Makoto
M
Nakama
Chisato
C
Kobayashi
Kensuke
K
Kawamoto
Hiroshi
H
Ito
Sayaka
S
Suzuki
Tomoki
T
Tani
Takeshi
T
Ozaki
Satoshi
S
Tokita
Shigeru
S
Sato
Nagaaki
N
D015761:4-Aminopyridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D000631:Aminopyridines / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D016466:CHO Cells; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D049268:Positron-Emission Tomography; D017476:Receptors, Neuropeptide Y / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry
D000631:Aminopyridines; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins; D013844:Thiazoles; C097212:neuropeptide Y-Y1 receptor; C026805:2,4-diaminopyridine; D015761:4-Aminopyridine