Discovery of a neuroprotective chemical, (S)- N -(3-(3,6-Dibromo-9 H -carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties

Jacinth Naidoo, Hector De Jesus-Cortes, Paula Huntington, Sandi Estill, Lorraine K. Morlock, Ruth Starwalt, Thomas J. Mangano, Noelle S. Williams, Andrew A. Pieper, Joseph M. Ready

Research output: Contribution to journalArticlepeer-review

38 Scopus citations

Abstract

(-)-P7C3-S243 is a neuroprotective aminopropyl carbazole with improved druglike properties compared with previously reported compounds in the P7C3 class. It protects developing neurons in a mouse model of hippocampal neurogenesis and protects mature neurons within the substantia nigra in a mouse model of Parkinsons disease. A short, enantioselective synthesis provides the neuroprotective agent in optically pure form. It is nontoxic, orally bioavailable, metabolically stable, and able to cross the blood-brain barrier. As such, it represents a valuable lead compound for the development of drugs to treat neurodegenerative diseases and traumatic brain injury.

Original languageEnglish (US)
Pages (from-to)3746-3754
Number of pages9
JournalJournal of Medicinal Chemistry
Volume57
Issue number9
DOIs
StatePublished - May 8 2014

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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