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Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors
Linköping University, Department of Physics, Chemistry and Biology, Chemistry. Linköping University, The Institute of Technology.
Medivir AB, Huddinge, Sweden.
Linköping University, Department of Physics, Chemistry and Biology, Chemistry. Linköping University, The Institute of Technology.
Medivir AB, Huddinge, Sweden.
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2015 (English)In: Open Medicinal Chemistry Journal, ISSN 1874-1045, Vol. 9, 13-26 p.Article in journal (Refereed) Published
Abstract [en]

A series of arylketo-containing P1-P3 linked macrocyclic BACE-1 inhibitors were designed, synthesized, and compared with compounds with a previously known and extensively studied corresponding P2 isophthalamide moiety with the aim to improve on permeability whilst retaining the enzyme- and cell-based activities. Several inhibitors displayed substantial increases in Caco-2 cell-based permeability compared to earlier synthesized inhibitors and notably also with retained activities, showing that this approach might yield BACE-1 inhibitors with improved properties.

Place, publisher, year, edition, pages
Bussum, Netherlands: Bentham Open , 2015. Vol. 9, 13-26 p.
Keyword [en]
Alzheimer’s disease, BACE-1 inhibition, cellular permeability, macrocycles, ring-closing metathesis, X-ray structure
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:liu:diva-120598DOI: 10.2174/1874104501509010013PubMedID: 25937848OAI: oai:DiVA.org:liu-120598DiVA: diva2:846750
Available from: 2015-08-18 Created: 2015-08-18 Last updated: 2017-12-04Bibliographically approved

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