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Tytuł pozycji:

Activity of Aromathecins against African Trypanosomes.

Tytuł:
Activity of Aromathecins against African Trypanosomes.
Autorzy:
Nenortas NP; Division of Clinical Pharmacology, Departments of Medicine and of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.
Cinelli MA; Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana, USA.
Morrell AE; Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana, USA.
Cushman M; Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana, USA.
Shapiro TA; Division of Clinical Pharmacology, Departments of Medicine and of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland, USA .
Źródło:
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2018 Oct 24; Vol. 62 (11). Date of Electronic Publication: 2018 Oct 24 (Print Publication: 2018).
Typ publikacji:
Journal Article; Research Support, N.I.H., Extramural
Język:
English
Imprint Name(s):
Original Publication: Washington, American Society for Microbiology
MeSH Terms:
Antiprotozoal Agents/*therapeutic use
Heterocyclic Compounds, 4 or More Rings/*therapeutic use
Trypanocidal Agents/*therapeutic use
Trypanosoma/*drug effects
Trypanosoma brucei brucei/*drug effects
Trypanosomiasis, African/*drug therapy
Humans ; Structure-Activity Relationship ; Trypanosomiasis, African/parasitology
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Grant Information:
R01 AI028855 United States AI NIAID NIH HHS; R01 AI095453 United States AI NIAID NIH HHS; R56 AI028855 United States AI NIAID NIH HHS; P30 CA023168 United States CA NCI NIH HHS; U01 CA089566 United States CA NCI NIH HHS
Contributed Indexing:
Keywords: Trypanosoma brucei; aromathecin; sleeping sickness; structure-activity; topoisomerase
Substance Nomenclature:
0 (Antiprotozoal Agents)
0 (Heterocyclic Compounds, 4 or More Rings)
0 (Trypanocidal Agents)
0 (rosettacin)
Entry Date(s):
Date Created: 20180815 Date Completed: 20191010 Latest Revision: 20191010
Update Code:
20240104
PubMed Central ID:
PMC6201061
DOI:
10.1128/AAC.00786-18
PMID:
30104277
Czasopismo naukowe
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.
(Copyright © 2018 American Society for Microbiology.)

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