Contilisant-Belinostat Hybrids: Polyfunctionalized Indole Derivatives as Multineurotarget Drugs for the Potential Treatment of Alzheimer's Disease.

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Tác giả: Sophia Eimermacher, Paul W Elsinghorst, Michael Gütschow, Finn K Hansen, Gabriele Horn, Vesa Krasniqi, José Marco-Contelles, Markus Pietsch, Alicia Porro-Pérez, Linda Schäker-Hübner, Philipp Stegen, Kathrin Tan, Mireia Toledano-Pinedo, Timo Wille

Ngôn ngữ: eng

Ký hiệu phân loại: 629.2507 Motor land vehicles, cycles

Thông tin xuất bản: United States : ACS pharmacology & translational science , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 724700

In this work, we designed, synthesized, and evaluated two types of multineurotargeting compounds using a pharmacophore merging strategy, aiming to develop potential treatments for Alzheimer's disease. We combined belinostat, an FDA-approved unselective histone deacetylase (HDAC) inhibitor, with the 5-substituted indole core of contilisant, known for its antioxidant and neuroprotective properties as well as its potent inhibitory activity against monoamine oxidases (MAOs), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Among these, compounds
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