Ontology highlight
ABSTRACT:
SUBMITTER: Zhang L
PROVIDER: S-EPMC4842970 | biostudies-literature | 2016 Apr
REPOSITORIES: biostudies-literature
Zhang Laitao L Li Yi-Fang YF Yuan Sheng S Zhang Shijie S Zheng Huanhuan H Liu Jie J Sun Pinghua P Gu Yijun Y Kurihara Hiroshi H He Rong-Rong RR Chen Heru H
Scientific reports 20160425
Bioactivity focus on α-cyano-4-hydroxycinnamic acid (CHCA) scaffold results in a small library of novel multifunctional aldose reductase (ALR2) inhibitors. All the entities displayed good to excellent inhibition with IC50 72-405 nM. (R,E)-N-(3-(2-acetamido-3-(benzyloxy)propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (5f) was confirmed as the most active inhibitor (IC50 72.7 ± 1.6 nM), and the best antioxidant. 5f bound to ALR2 with new mode without affecting the aldehyde reductase (AL ...[more]