Design and synthesis of potent and selective BACE-1 inhibitors
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
Several highly potent BACE-1 protease inhibitors have been developed from an inhibitor series containing a novel hydroxyethylene (HE) core structure displaying aryloxymethyl or benzyloxymethyl P1 side chains and a methoxy P1’ side chain. The target molecules were readily synthesized from chiral carbohydrate starting materials, furnishing the inhibitor compounds in good overall yields. The inhibitors show both high BACE-1 potency and good selectivity against cathepsin D, where the most potent inhibitor furnish a BACE-1 IC50 value of 0.32 nM and displays > 3000 fold selectivity over cathepsin D.
Place, publisher, year, edition, pages
American Chemical Society , 2010. Vol. 53, no 4, 1458-1464 p.
Research subject Organic Chemistry
IdentifiersURN: urn:nbn:se:su:diva-29748DOI: 10.1021/jm901168fISI: 000274581200004OAI: oai:DiVA.org:su-29748DiVA: diva2:235025