Synthesis and preliminary biological evaluation of new α-amino amide anticonvulsants incorporating a dextromethorphan moiety

Paolo Pevarello, Gabriella Traquandi, Alberto Bonsignori, Robert A. McArthur, Roberto Maj, Carla Caccia, Patricia Salvati, Mario Varasi

Research output: Contribution to journalArticle

Abstract

Dextromethorphan 1 is an effective neuroprotectant in animal models of epilepsy and ischemia but showed side-effects during clinical trials limiting its potential use in a clinical setting. Here we describe the enantioselective and enantiospecific syntheses and the initial in vitro and in vivo biological evaluation of new hybrid structures between 1 and a previously disclosed α-amino amide anticonvulsant (3).

Original languageEnglish
Pages (from-to)1783-1788
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume9
Issue number13
DOIs
Publication statusPublished - Jul 5 1999

Keywords

  • Amino acids and derivs
  • Anticonvulsants
  • Neurologically active compds
  • Stereospecificity

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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