Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

(1 ,4 )-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 -pentyl and -methylenethiophene substituted analogs 11g and 11h emerged as s...

Full description

Saved in:
Bibliographic Details
Published in:MedChemComm 2013-07, Vol.4 (7), p.1085-1092
Main Authors: Cifuentes-Pagano, Eugenia, Saha, Jaideep, Csányi, Gábor, Ghouleh, Imad Al, Sahoo, Sanghamitra, Rodríguez, Andrés, Wipf, Peter, Pagano, Patrick J, Skoda, Erin M
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:(1 ,4 )-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 -pentyl and -methylenethiophene substituted analogs 11g and 11h emerged as selective Nox2 inhibitors with cellular IC values of 20 and 32 μM, respectively.
ISSN:2040-2503
2040-2511
DOI:10.1039/c3md00061c