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

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

Research output: Contribution to journalArticle

15 Scopus citations

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 2013

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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    Cifuentes-Pagano, E., Saha, J., Csányi, G., Al Ghouleh, I., Sahoo, S., Rodríguez, A., Wipf, P., Pagano, P. J., & 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