Abstract
In order to develop small molecular probes for imaging of Aβ plaques in the brain with Alzheimer’s disease, four benzothiazole derivatives as Aβ probes, 3’-125I-BTA, 3’-125I-CBTA, 3’-125I-BTA-Ac, and 3’-125I-CBTA-Ac were successfully prepared. The four probes displayed the following initial brain uptake: 10.28 %ID/g, 3.62 %ID/g, 3.33 %ID/g and 3.71 %ID/g at 2-minute post iv injection, respectively. The study of quantitative structure-activity relationship (QSAR) indicated that the initial brain uptake was correlated with molecule volume (Vm) and dipole moment (Dp), but the Dp was the main factor. 3’-125I-BTA has the highest initial brain uptake among the four Aβ probes because of the smallest Dp.
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