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Aurones : A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents
Joint Authors
Kypreou, Anna-Maria
Cordeiro da Silva, Anabela
Roussaki, Marina
Detsi, Anastasia
Costa Lima, Sofia
Kefalas, Panagiotis
Source
International Journal of Medicinal Chemistry
Issue
Vol. 2012, Issue 2012 (31 Dec. 2012), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2012-09-25
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
A series of (Z)-2-benzylidenebenzofuran-3-(2H)-ones (aurones) bearing a variety of substituents on rings A and B were synthesized and evaluated for their antiparasitic activity against the intracellular amastigote form of Leishmania infantum and their cytotoxicity against human THP1-differentiated macrophages.
In general, aurones bearing no substituents on ring A (compounds 4a–4f) exhibit higher toxicity than aurones with 4,6-dimethoxy substitution (compounds 4g–4l).
Among the latter, two aurones possessing a 2′-methoxy or a 2′-methyl group (compounds 4i and 4j) exhibit potent antileishmanial activity (IC50=1.3±0.1 μM and IC50=1.6±0.2 μM, resp.), comparable to the activity of the reference drug Amphotericin B, whereas they present significantly lower cytotoxicity than Amphotericin B as deduced by the higher selectivity index.
American Psychological Association (APA)
Roussaki, Marina& Costa Lima, Sofia& Kypreou, Anna-Maria& Kefalas, Panagiotis& Cordeiro da Silva, Anabela& Detsi, Anastasia. 2012. Aurones : A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents. International Journal of Medicinal Chemistry،Vol. 2012, no. 2012, pp.1-8.
https://search.emarefa.net/detail/BIM-453744
Modern Language Association (MLA)
Roussaki, Marina…[et al.]. Aurones : A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents. International Journal of Medicinal Chemistry No. 2012 (2012), pp.1-8.
https://search.emarefa.net/detail/BIM-453744
American Medical Association (AMA)
Roussaki, Marina& Costa Lima, Sofia& Kypreou, Anna-Maria& Kefalas, Panagiotis& Cordeiro da Silva, Anabela& Detsi, Anastasia. Aurones : A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents. International Journal of Medicinal Chemistry. 2012. Vol. 2012, no. 2012, pp.1-8.
https://search.emarefa.net/detail/BIM-453744
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-453744