Synthesis and Evaluation of 18F-Labeled Styryltriazole and Resveratrol Derivatives for β-Amyloid Plaque Imaging

I Lee, YS Choe, JY Choi, KH Lee…

Index: Lee, Iljung; Choe, Yearn Seong; Choi, Joon Young; Lee, Kyung-Han; Kim, Byung-Tae Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 883 - 892

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Citation Number: 20

Abstract

In the present study, a styryltriazole and four resveratrol derivatives were synthesized as candidates for β-amyloid (Aβ) plaque imaging. On the basis of their binding affinities to Aβ (1– 42) aggregates, the styryltriazole (1, K i= 12.8 nM) and one resveratrol derivative (5, K i= 0.49 nM) were labeled with 18F. In normal mice, tissue distribution of [18F] 5 showed good initial brain uptake (3.26% ID/g at 2 min) but slow wash-out from brains (2-to-60 min ...