4.5 Article

Discovery of sulfonamide-pyrazole γ-secretase inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 7, Pages 2148-2150

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.050

Keywords

Alzheimer's disease; gamma-secretase inhibitor; Sulfonamide

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Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance. (C) 2010 Elsevier Ltd. All rights reserved.

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