Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors

Eugenia Cifuentes-Pagano, Jaideep Saha, Gabor Csanyi, Imad Al Ghouleh, Sanghamitra Sahoo, Andrés Rodríguez, Peter Wipf, Patrick J. Pagano, Erin M. Skoda

Research output: Contribution to journalArticle

10 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)1085-1092
Number of pages8
JournalMedChemComm
Volume4
Issue number7
DOIs
StatePublished - Jul 1 2013

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Naphthalenes
Tetrahydroisoquinolines
NADPH Oxidase
Inhibitory Concentration 50
Protein Isoforms

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

Cifuentes-Pagano, E., Saha, J., Csanyi, G., Al Ghouleh, I., Sahoo, S., Rodríguez, A., ... Skoda, E. M. (2013). Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors. MedChemComm, 4(7), 1085-1092. https://doi.org/10.1039/c3md00061c

Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors. / Cifuentes-Pagano, Eugenia; Saha, Jaideep; Csanyi, Gabor; Al Ghouleh, Imad; Sahoo, Sanghamitra; Rodríguez, Andrés; Wipf, Peter; Pagano, Patrick J.; Skoda, Erin M.

In: MedChemComm, Vol. 4, No. 7, 01.07.2013, p. 1085-1092.

Research output: Contribution to journalArticle

Cifuentes-Pagano, E, Saha, J, Csanyi, G, Al Ghouleh, I, Sahoo, S, Rodríguez, A, Wipf, P, Pagano, PJ & Skoda, EM 2013, 'Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors', MedChemComm, vol. 4, no. 7, pp. 1085-1092. https://doi.org/10.1039/c3md00061c
Cifuentes-Pagano E, Saha J, Csanyi G, Al Ghouleh I, Sahoo S, Rodríguez A et al. Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors. MedChemComm. 2013 Jul 1;4(7):1085-1092. https://doi.org/10.1039/c3md00061c
Cifuentes-Pagano, Eugenia ; Saha, Jaideep ; Csanyi, Gabor ; Al Ghouleh, Imad ; Sahoo, Sanghamitra ; Rodríguez, Andrés ; Wipf, Peter ; Pagano, Patrick J. ; Skoda, Erin M. / Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox 2) inhibitors. In: MedChemComm. 2013 ; Vol. 4, No. 7. pp. 1085-1092.
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