Design and synthesis of novel macrocyclic BACE-1 inhibitors
(English)Manuscript (preprint) (Other academic)
A series of arylketo-containing P1-P3 linked macrocyclic inhibitors was designed and synthesized and compared with a previously known and extensively used corresponding P2 isophthalamide moiety with the aim to improve on permeability whilst retaining the enzyme and cell-based potencies. Several inhibitors displayed a substantial increase in Caco-2 cell-based permeability and notably also with retained potencies, showing that this approach might lead to centrally active BACE-1 inhibitors.
IdentifiersURN: urn:nbn:se:liu:diva-76173OAI: oai:DiVA.org:liu-76173DiVA: diva2:512920