Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors
2015 (English)In: Open Medicinal Chemistry Journal, ISSN 1874-1045, Vol. 9, 13-26 p.Article in journal (Refereed) Published
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.
Alzheimer’s disease, BACE-1 inhibition, cellular permeability, macrocycles, ring-closing metathesis, X-ray structure
IdentifiersURN: urn:nbn:se:liu:diva-120598DOI: 10.2174/1874104501509010013PubMedID: 25937848OAI: oai:DiVA.org:liu-120598DiVA: diva2:846750