首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.
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Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.

机译:新的(2E,6E)-10-(二甲基氨基)-3,7-二甲基-2,6-癸二烯-1-醇醚作为人和锥虫克鲁兹氧化角鲨烯环化酶抑制剂的设计,合成和生物学评估。

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摘要

New dimethylamino truncated squalene ether derivatives containing a different aromatic moiety (phenyl, naphthyl, and biphenyl) or a simple alkyl (n-hexylic) group were synthesized as inhibitors of the oxidosqualene cyclase (OSC) and of the sterol biosynthetic pathway. The activity against human OSC was compared with the activity against the OSCs of pathogenic organisms such as Pneumocystis carinii and Trypanosoma cruzi. The phenyl derivative was the most potent inhibitor of T. cruzi OSC.
机译:合成了具有不同芳族部分(苯基,萘基和联苯)或简单烷基(正己基)基团的新二甲氨基截短的角鲨烯醚衍生物,作为氧化角鲨烯环化酶(OSC)和固醇生物合成途径的抑制剂。将针对人OSC的活性与诸如卡氏肺孢子虫和克氏锥虫的致病生物的针对OSC的活性进行了比较。苯基衍生物是克鲁维酵母OSC的最有效抑制剂。

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