4.5 Article

Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positions

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 11, 页码 3447-3451

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.094

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gamma-Secretase inhibitor; Tricyclic sulfones; Alzheimer's disease

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SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modification resulted in new tricyclic sulfone analogs with efficacy in in vivo mouse A beta(40) lowering model. (C) 2011 Elsevier Ltd. All rights reserved.

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