Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

Cifuentes-Pagano, E; Saha, J; Csanyi, G; Al Ghouleh, I; Sahoo S.; Rodríguez A.; Wipf, P; Pagano, PJ; Skoda, EM

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