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 μM, respectively.

SUBMITTER: Cifuentes-Pagano E 

PROVIDER: S-EPMC3897123 | biostudies-literature | 2013 Jul

REPOSITORIES: biostudies-literature