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Design and Synthesis of Potent and Selective BACE-1 Inhibitors
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2010 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 53, no 4, 1458-1464 p.Article in journal (Refereed) Published
Abstract [en]

Highly potent BACE-1 protease inhibitors have been developed from ill inhibitors containing a hydroxyethylene (HE) core displaying aryloxymethyl or benzyloxymethyl P1 side chain and a methoxy P1' side chain. The target molecules were synthesized in good overall yields from chiral carbohydrate starting materials. The inhibitors show high BACF-1 potency and good selectivity against cathepsin D, where the most potent inhibitor Furnishes BACE-1 Ki << 1 nM and displays > 1000-fold selectivity over cathepsin D.

Place, publisher, year, edition, pages
2010. Vol. 53, no 4, 1458-1464 p.
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-137302DOI: 10.1021/jm901168fISI: 000274581200004PubMedID: 20128595OAI: oai:DiVA.org:uu-137302DiVA: diva2:378159
Available from: 2010-12-15 Created: 2010-12-15 Last updated: 2010-12-15Bibliographically approved

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