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Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei.
- Source :
-
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2016 Mar 25; Vol. 60 (4), pp. 2532-6. Date of Electronic Publication: 2016 Mar 25 (Print Publication: 2016). - Publication Year :
- 2016
-
Abstract
- Current treatments for African trypanosomiasis are either toxic, costly, difficult to administer, or prone to elicit resistance. This study evaluated the activity of bisnaphthalimidopropyl (BNIP) derivatives againstTrypanosoma brucei BNIPDiaminobutane (BNIPDabut), the most active of these compounds, showedin vitroinhibition in the single-unit nanomolar range, similar to the activity in the reference drug pentamidine, and presented low toxicity and adequate metabolic stability. Additionally, using a murine model of acute infection and live imaging, a significant decrease in parasite load in BNIPDabut-treated mice was observed. However, cure was not achieved. BNIPDabut constitutes a new scaffold for antitrypanosomal drugs that deserves further consideration.<br /> (Copyright © 2016, American Society for Microbiology. All Rights Reserved.)
- Subjects :
- Animals
Cell Line
Drug Stability
Female
Hepatocytes cytology
Hepatocytes drug effects
Hepatocytes metabolism
Humans
Inhibitory Concentration 50
Liver drug effects
Liver metabolism
Macrophages cytology
Macrophages drug effects
Macrophages metabolism
Mice
Mice, Inbred BALB C
Microsomes, Liver drug effects
Microsomes, Liver metabolism
Mitochondria, Liver drug effects
Mitochondria, Liver metabolism
Naphthalimides chemical synthesis
Neurons cytology
Neurons drug effects
Neurons metabolism
Parasite Load
Pentamidine pharmacology
Primary Cell Culture
Structure-Activity Relationship
Survival Analysis
Trypanocidal Agents chemical synthesis
Trypanosoma brucei brucei growth & development
Trypanosoma brucei brucei metabolism
Trypanosomiasis, African mortality
Trypanosomiasis, African parasitology
Trypanosomiasis, African pathology
Naphthalimides pharmacology
Trypanocidal Agents pharmacology
Trypanosoma brucei brucei drug effects
Trypanosomiasis, African drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1098-6596
- Volume :
- 60
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Antimicrobial agents and chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 26787703
- Full Text :
- https://doi.org/10.1128/AAC.02490-15