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首页> 外文期刊>RSC Advances >Discovery of cytochrome bc1 complex inhibitors inspired by the natural product karrikinolide
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Discovery of cytochrome bc1 complex inhibitors inspired by the natural product karrikinolide

机译：通过天然产品Karrikinolide发现的细胞色素BC1复杂抑制剂的发现

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The cytochrome bc _(1) complex (cyt bc _(1) or complex III) is a promising target of numerous antibiotics and fungicides. With an aim to indentify new lead structures for the bc _(1) complex, a series of novel inhibitors were discovered from the natural product karrikinolide for the first time. Extensive screening results suggested variable inhibitory activities of these compounds against succinate-cytochrome reductase [SCR, a mixture of respiratory complex II (SQR) and complex III (the bc _(1) complex)], implying the essential role of a 4-substituted phenyl group for the high potency. Exceptionally, compound 12g showed excellent inhibition potency having an IC _(50) value in the sub-micromolar range, demonstrating its higher potency than the commercial control amisulbrom by over two orders of magnitude. Further experiments inferred that these newly prepared compounds mainly target the bc _(1) complex. Seemingly, this work has presented a new lead scaffold for further development of bc _(1) complex inhibitors.
机译：细胞色素Bc _（1）复合物（Cyt Bc _（1）或复合III）是许多抗生素和杀菌剂的有希望的靶标。目的是依附于BC _（1）复合物的新铅结构，首次从天然产物Karrikinolide发现一系列新的抑制剂。广泛的筛选结果提出了这些化合物对琥珀酸酯 - 细胞色素还原酶的可变抑制活性[SCR，呼吸道复合物II（SQR）和复合物III的混合物（BC _（1）复合物）]，暗示了4个取代的基本作用苯基用于高效力。特别地，化合物12G在亚微摩尔范围内显示出具有IC _（50）值的优异的抑制效力，其比商业对照Amusulbrom在两种数量级上显示其较高效力。进一步的实验推断出这些新制备的化合物主要靶向BC _（1）复合物。似乎，这项工作提出了一种新的铅脚手架，用于进一步发展BC _（1）复合抑制剂。

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