Design, synthesis and biological evaluation of air-stable nafuredin-γ analogs as complex II inhibitors.
Design, synthesis and biological evaluation of air-stable nafuredin-γ analogs as complex II inhibitors.
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作为复合物 II 抑制剂的空气稳定 nafuredin-γ 类似物的设计、合成和生物学评价。
DOI：
10.1016/j.bmc.2015.01.030
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发表时间：
2015
期刊：
影响因子：
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通讯作者：
S.; Nagamitsu. T.
中科院分区：
文献类型：
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作者：
Ohtawa;M.; Matsunaga;M.; Fukunaga;K.; Shimizu;R.; Shimizu;E.; Arima;S.; Ohmori;J.; Kita;K.; Shiomi;K.; Omura;S.; Nagamitsu. T.
萘呋啶-γ（2）是萘呋啶（1）在温和碱性条件下转化而成的，对蠕虫复合物I显示出有效和选择性的抑制活性。然而，2在空气中是不稳定的，因为共轭二烯是氧不稳定的。为了解决这个问题，我们设计并合成了空气稳定的萘呋啶-γ类似物。尽管所有新萘呋啶-γ类似物的复合物I抑制活性均低于2的复合物I抑制活性，但所有复合物I抑制活性均在高nM范围内（IC 50：300-820 nM）。
Nafuredin-γ (2), converted from nafuredin (1) under mild basic conditions, demonstrates potent and selective inhibitory activity against helminth complex I. However,2is unstable in air because the conjugated dienes are oxygen-labile. To address this, we designed and synthesized air-stable nafuredin-γ analogs. Although the complex I inhibitory activities of all the new nafuredin-γ analogs were lower than that of2, all were in the high nM range (IC50: 300–820 nM).