期刊
INTERNATIONAL JOURNAL OF MEDICINAL CHEMISTRY
卷 2012, 期 -, 页码 -出版社
HINDAWI LTD
DOI: 10.1155/2012/196921
关键词
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资金
- Fundacao para a Ciencia e Tecnologia (FCT) [SFRH/BPD/37880/2007]
- FSE (III Quadro Comunitario) [SFRH/BPD/37880/2007]
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 formof 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 mu M and IC50 = 1.6 +/- 0.2 mu M, 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.
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