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Evaluation of trypanocidal and antioxidant activities of a selected series of 3-amidocoumarins

dc.contributor.authorMoncada-Basualto M.
dc.contributor.authorLapier M.
dc.contributor.authorMaya J.D.
dc.contributor.authorMatsuhiro B.
dc.contributor.authorOlea-Azar C.
dc.contributor.authorDelogu G.L.
dc.contributor.authorUriarte E.
dc.contributor.authorSantana L.
dc.contributor.authorMatos M.J.
dc.date.accessioned2020-09-02T22:23:31Z
dc.date.available2020-09-02T22:23:31Z
dc.date.issued2018
dc.identifier10.2174/1573406414666180419113437
dc.identifier.citation14, 6, 573-584
dc.identifier.issn15734064
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5381
dc.descriptionBackground: Neglected diseases are becoming more prevalent due to globalization. This has inspired active research in the development of new drugs for the treatment of parasitic diseases such as Chagas disease. Objectives: With the aim of finding new trypanocidal agents, we report the in vitro evaluation of a new series of 3-amidocoumarins with or without hydroxyl substituents at position 4 of the coumarin ring. Methods: Electrochemical and biological assays were performed in order to assess the antioxidant and trypanocidal potential of these compounds and to better understand the mechanisms involved in their activity. Results: Most of the studied compounds showed high trypanocidal activity against both epimastigote and trypomastigote forms, with IC50 values in the low micromolar range. Some of them have greater activity and selectivity than the reference compound, nifurtimox. Conclusion: Compound 2 is the most active of this series, being also non-cytotoxic against murine RAW 264.7 macrophages. Electrochemical and radical scavenging experiments were carried out, providing new information about the profile of the best derivatives, and the potential therapeutic application of the new 3-amidocoumarins. © 2018 Bentham Science Publishers.
dc.language.isoen
dc.publisherBentham Science Publishers B.V.
dc.subject3-Amidocoumarins
dc.subjectAntioxidant
dc.subjectChagas disease
dc.subjectProtozoan parasite
dc.subjectTrypanocidal
dc.subjectTrypanosoma cruzi
dc.subject3 amidocoumarin
dc.subjectantitrypanosomal agent
dc.subjectcoumarin derivative
dc.subjectnifurtimox
dc.subjecttrolox C
dc.subjectunclassified drug
dc.subject6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
dc.subjectamide
dc.subjectantioxidant
dc.subjectantitrypanosomal agent
dc.subjectchroman derivative
dc.subjectcoumarin derivative
dc.subjectfree radical
dc.subjectnifurtimox
dc.subjectantioxidant activity
dc.subjectArticle
dc.subjectChagas disease
dc.subjectchromatography
dc.subjectcontrolled study
dc.subjectcyclic potentiometry
dc.subjectdifferential pulse voltammetry
dc.subjectdrug adsorption
dc.subjectelectron spin resonance
dc.subjectenergy balance
dc.subjectepimastigote
dc.subjectin vitro study
dc.subjectmitochondrial membrane potential
dc.subjectnonhuman
dc.subjectoxidation reduction potential
dc.subjectoxidative stress
dc.subjectoxygen radical absorbance capacity
dc.subjectpriority journal
dc.subjectRAW 264.7 cell line
dc.subjecttrypomastigote
dc.subjectanimal
dc.subjectchemical model
dc.subjectchemical structure
dc.subjectchemistry
dc.subjectdrug sensitivity
dc.subjectelectrochemical analysis
dc.subjectmouse
dc.subjectsynthesis
dc.subjectAmides
dc.subjectAnimals
dc.subjectAntioxidants
dc.subjectChromans
dc.subjectCoumarins
dc.subjectElectrochemical Techniques
dc.subjectFree Radicals
dc.subjectMice
dc.subjectModels, Chemical
dc.subjectMolecular Structure
dc.subjectNifurtimox
dc.subjectParasitic Sensitivity Tests
dc.subjectRAW 264.7 Cells
dc.subjectTrypanocidal Agents
dc.titleEvaluation of trypanocidal and antioxidant activities of a selected series of 3-amidocoumarins
dc.typeArticle


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