1.
Bioorg Med Chem
; 23(17): 5352-9, 2015 Sep 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26278028
RESUMO
Nrf2 activators represent a good drug target for designing agents to treat diseases associated with oxidative stress. Building upon previous work, we designed and prepared a series of heterocyclic chalcone-based Nrf2 activators with reduced lipophilicity and, in some cases, greater in vitro potency compared to the respective carbocyclic scaffold. These changes resulted in enhanced oral bioavailability and a superior pharmacodynamic effect in vivo.