New pyrano‐4H‐benzo[g]chromene‐5,10‐diones with anti‐parasitic and anti‐oxidant activities,Chemistry & Biodiversity

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New pyrano‐4H‐benzo[g]chromene‐5,10‐diones with anti‐parasitic and anti‐oxidant activities
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-12-17 , DOI: 10.1002/cbdv.202000839
Ibrahim S Al Nasr _{1,

2} , Jana Jentzsch ₃ , Amin Shaikh ₄ , Priti Singh Shuveksh ₄ , Waleed S Koko ₂ , Tariq A Khan ₅ , Khursheed Ahmed ₄ , Rainer Schobert ₆ , Klaus Ersfeld ₃ , Bernhard Biersack ₆

Affiliation

New pyranonaphthoquinone derivatives were synthesized and investigated for their activity against Trypanosoma brucei, Leishmania major, and Toxoplasma gondii parasites. The pentafluorophenyl derivative was efficacious against T. brucei with single digit micromolar EC50 values and against T. gondii with even sub‐micromolar values. The 3‐chloro‐4,5‐dimethoxyphenyl derivative showed an activity against amastigotes of Leishmania major parasites comparable to that of amphotericin B. In addition, antioxidant activities were observed for the bromophenyl derivatives, and their redox behavior was studied by cyclovoltammetry. Anti‐parasitic and antioxidative activities of the new naphthoquinone derivatives appear uncorrelated.

中文翻译：

具有抗寄生虫和抗氧化活性的新型吡喃-4H-苯并[g]色烯-5,10-二酮

合成了新的吡喃萘醌衍生物并研究了它们对布氏锥虫、主要利什曼原虫和弓形虫寄生虫的活性。五氟苯基衍生物对具有个位数微摩尔 EC50 值的布氏锥虫有效，甚至对亚微摩尔值的刚地弓形虫有效。3-氯-4,5-二甲氧基苯基衍生物对利什曼原虫主要寄生虫的无鞭毛体具有与两性霉素 B 相当的活性。此外，观察到溴苯基衍生物的抗氧化活性，并通过循环伏安法研究了它们的氧化还原行为。新萘醌衍生物的抗寄生虫和抗氧化活性似乎不相关。

更新日期：2020-12-17

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