Synthesis and Characterization of Lipophilic 1-(18F) Fluoroalkyl-2-nitroimidazoles for Imaging Hypoxia.

…, S Antoku, Y Ichiya, K MASUDA, M MAEDA

Index: Yamamoto, Fumihiko; Oka, Hidenobu; Antoku, Shigetoshi; Ichiya, Yu-Ichi; Masuda, Kouji; Maeda, Minoru Biological and Pharmaceutical Bulletin, 1999 , vol. 22, # 6 p. 590 - 597

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Citation Number: 26

Abstract

In order to develop new imaging markers for brain hypoxia, two lipophilic nitroimidazoles, 1- (3-fluoropropyl)-2-nitroimidazole (FPN) and 1-(8-fluorooctyl)-2-nitroimidazole (FON) were synthesized and labeled with fluorine-18. The octanol/water partition coefficients were measured as an indication of lipophilicity, giving values of log P= 0.28 for FPN and log P= 2.72 for FON, respectively, which are in the range thought to be optimal for the diffusion of ...