4.5 Article

Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure-activity relationship studies

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 12, Pages 3632-3635

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.104

Keywords

gamma-Secretase; Alzheimer's disease; Sulfone

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Tricyclic sulfones were designed as gamma-secretase inhibitors and found to have excellent potency. Extensive SAR shows that a large number of sulfonamides at position 7 of the tricycle are very well tolerated. Compounds such as 15a and 15c showed remarkable in vivo potency. (C) 2010 Elsevier Ltd. All rights reserved.

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