Synthesis and evaluation of three 18F-labeled aminophenylbenzothiazoles as amyloid imaging agents

K Serdons, K Van Laere, P Janssen…

Index: Serdons, Kim; Van Laere, Koen; Janssen, Peter; Kung, Hank F.; Bormans, Guy; Verbruggen, Alfons Journal of Medicinal Chemistry, 2009 , vol. 52, # 22 p. 7090 - 7102

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Citation Number: 16

Abstract

We have developed three fluorine-18 labeled 6-(methyl) amino-2-(4′-fluorophenyl)-1, 3- benzothiazoles, which display high in vitro binding affinity for human amyloid β plaques (K i≤ 10 nM). The radiolabeled probes were synthesized by aromatic nucleophilic substitution of the corresponding nitro precursor with 18F-fluoride, followed by deprotection of the BOC group if required. Determination of the octanol/water partition coefficient, biodistribution ...