Activity of Aromathecins against African Trypanosomes

Nathaniel P. Nenortas, Maris A. Cinelli, Andrew E. Morrell, Mark Cushman, Theresa A Shapiro

Research output: Contribution to journalArticle

Abstract

African sleeping sickness is responsible for thousands of deaths annually, and new therapeutics are needed. This study evaluated aromathecins, experimental inhibitors of mammalian topoisomerase IB, against Trypanosoma brucei African trypanosomes. The compounds had selectively toxic antiparasitic potency, in situ poisoning activity against the phylogenetically unique topoisomerase in these parasites, and a representative compound intercalated into DNA with micromolar affinity. DNA intercalation and topoisomerase poisoning may contribute to the antitrypanosomal activity of aromathecins.

Original languageEnglish (US)
JournalAntimicrobial Agents and Chemotherapy
Volume62
Issue number11
DOIs
StatePublished - Nov 1 2018

Keywords

  • aromathecin
  • sleeping sickness
  • structure-activity
  • topoisomerase
  • Trypanosoma brucei

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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