In vitro antileishmanial activity of trans-stilbene and terphenyl compounds.
作者： Germano Castelli , Federica Bruno , Fabrizio Vitale , Marinella Roberti , Claudia Colomba
DOI: 10.1016/J.EXPPARA.2016.03.007
关键词: Leishmaniasis 、 Terphenyl Compounds 、 Leishmania infantum 、 Terphenyl 、 Structure–activity relationship 、 Amastigote 、 Pharmacology 、 Immunology 、 In vitro 、 Context (language use) 、 Biology
摘要: Leishmaniasis are globally widespread parasitic diseases which often leads to death if left untreated. Currently available drugs present different drawbacks, so there is an urgent need develop new, safe and cost-effective against leishmaniasis. In this study we tested a small library of trans-stilbene terphenyl derivatives promastigote, amastigotes intramacrophage amastigote forms Leishmania infantum. Two compounds the series, 3 11, presented best activity safety profiles. Terphenyl 11 showed leshmanicidal higher than pentostam ability induce apoptosis selectively in infantum while saving macrophages primary epithelial cells. Our data indicate that compounds, as well stilbenes, endowed with leishmanicidal activity, showing potential for further studies context leishmanial therapy.
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