Issue 7, 2013
From the journal:

MedChemComm

Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors†

Eugenia Cifuentes-Pagano,a   Jaideep Saha,ab   Gábor Csányi,a   Imad Al Ghouleh,a   Sanghamitra Sahoo,a   Andrés Rodríguez,a   Peter Wipf,bc   Patrick J. Pagano*a  and  Erin M. Skoda*b  

* Corresponding authors

a Vascular Medicine Institute, Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA
E-mail: pagano@pitt.edu

b Center for Chemical Methodologies and Library Development, Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15261, USA
E-mail: emf53@pitt.edu

c Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA

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.

Graphical abstract: Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

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Article information

DOI
https://doi.org/10.1039/C3MD00061C
Article type
Concise Article
Submitted
25 Feb 2013
Accepted
22 May 2013
First published
05 Jun 2013

Med. Chem. Commun., 2013,4, 1085-1092

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Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors

E. Cifuentes-Pagano, J. Saha, G. Csányi, I. Al Ghouleh, S. Sahoo, A. Rodríguez, P. Wipf, P. J. Pagano and E. M. Skoda, Med. Chem. Commun., 2013, 4, 1085 DOI: 10.1039/C3MD00061C

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