One-pot, multicomponent synthesis of 2,3-disubstituted quinazolin-ones with potent and selective activity against Toxoplasma gondii

Carla E. Brown, Tiffany Kong, Claudia Bordón, Robert H Yolken, Lorraine V Brando, James McNulty

Research output: Contribution to journalArticle

Abstract

The discovery of two quinazolinones with selective, single-digit micromolar activity (IC50 = 6–7 µM) against the tachyzoites of the apicomplexan parasite Toxoplasma gondii is reported. These potent and selective third generation derivatives contain a benzyloxybenzyl substituent at C2 and a bulky aliphatic moiety at N3. Here we show that these quinazolinones inhibit T. gondii tachyzoite replication in an established infection, but do not significantly affect host cell invasion by the tachyzoites.

Original languageEnglish (US)
JournalBioorganic and Medicinal Chemistry Letters
DOIs
StateAccepted/In press - Jan 1 2018

Keywords

  • Multi-component synthesis
  • Quinazolinone
  • Toxoplasma gondii
  • Toxoplasmosis

ASJC Scopus subject areas

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

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