Ontology highlight
ABSTRACT:
SUBMITTER: Sandgren V
PROVIDER: S-EPMC4412958 | biostudies-literature | 2015
REPOSITORIES: biostudies-literature
The open medicinal chemistry journal 20150331
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 th ...[more]