Antiprotozoal Selectivity of Diimidazoline N-Phenylbenzamides

Xiaofang Wang, Yuxiang Dong, Monica Cal, Marcel Kaiser, Sergio Wittlin, Jonathan L. Vennerstrom

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

We discovered three diimidazolines with high antiplasmodial selectivity that had IC50 values of 1.9-28 nM against cultured Plasmodium falciparum. We also identified a gem-dimethyl diimidazoline with high antitrypanosomal selectivity that had an IC50 value of 26 nM against cultured Trypanosoma brucei rhodesiense. Two 2-imidazoline heterocycles in a para orientation on a N-phenylbenzamide or similar core structure were required for high antiprotozoal activity. Ring expansion of the imidazoline as well as heterocyclic variants with pKa values of <7 all decreased activity significantly.

Original languageEnglish (US)
Pages (from-to)135-139
Number of pages5
JournalACS infectious diseases
Volume1
Issue number3
DOIs
StatePublished - Jan 8 2016

Keywords

  • N-phenylbenzamide
  • antimalarial
  • antiprotozoal
  • antitrypanosomal
  • diamidine
  • diimidazoline

ASJC Scopus subject areas

  • Infectious Diseases

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