Activity of Aromathecins against African Trypanosomes.

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.

• Authors: Nathaniel P Nenortas, Maris A Cinelli, Andrew E Morrell, Mark Cushman, Theresa A Shapiro
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 62 Issue 11 (11 2018) ISSN: 1098-6596 [Electronic] United States
• PMID: 30104277 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
• Copyright: Copyright © 2018 American Society for Microbiology.

Chemical References

• Antiprotozoal Agents
• Heterocyclic Compounds, 4 or More Rings
• Trypanocidal Agents
• rosettacin

Topics

• Antiprotozoal Agents (therapeutic use)
• Heterocyclic Compounds, 4 or More Rings (therapeutic use)
• Humans
• Structure-Activity Relationship
• Trypanocidal Agents (therapeutic use)
• Trypanosoma (drug effects)
• Trypanosoma brucei brucei (drug effects)
• Trypanosomiasis, African (drug therapy, parasitology)