Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
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ABSTRACT:
SUBMITTER: Cifuentes-Pagano E
PROVIDER: S-EPMC3897123 | biostudies-literature | 2013 Jul
REPOSITORIES: biostudies-literature
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Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
Cifuentes-Pagano Eugenia E Saha Jaideep J Csányi Gábor G Ghouleh Imad Al IA Sahoo Sanghamitra S Rodríguez Andrés A Wipf Peter P Pagano Patrick J PJ Skoda Erin M EM
MedChemComm 20130701 7
(1<i>SR</i>,4<i>RS</i>)-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 <i>N</i>-pentyl and <i>N</i>-methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC<sub>50</sub> values of 20 and 32 μM, respectively. ...[more]
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