Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors
Abstract
(1SR,4RS)-3,3-Dimethyl-1,2,3,4-tetrahydro-1,4-(epiminomethano)naphthalenes were synthesized in 2-3 steps from commercially available materials and assessed for specificity and effectiveness across a range of Nox isoforms. The N-pentyl and N-methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC50 values of 20 and 32 mu M, respectively.
Más información
Título según WOS: | Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors |
Título de la Revista: | MEDCHEMCOMM |
Volumen: | 4 |
Número: | 7 |
Editorial: | ROYAL SOC CHEMISTRY |
Fecha de publicación: | 2013 |
Página de inicio: | 1085 |
Página final: | 1092 |
Idioma: | English |
DOI: |
10.1039/c3md00061c |
Notas: | ISI |