Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor

Ohtawa Masaki; Arima Shiho; Shimizu Risa; Hanatani Naomi; Shimizu Eri; Shiomi Kazuro; Kita Kiyoshi; Omura Satoshi; Nagamitsu Tohru

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Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor

机译：开发新的空气稳定结构简化的Nafuredin-Gamma模拟，作为有效和选择性线性复合物I抑制剂

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Nafuredin-gamma, obtained from natural nafuredin, has demonstrated a potent and selective inhibitory activity against nematode complex I. However, nafuredin-gamma is unstable in air since its conjugated dienes are oxygen-labile. The instability in air was naturally solved by the synthesis of structure-simplified nafuredin-gamma analogs without conjugated dienes. However, these modified analogs showed lower complex I inhibitory activities. Therefore, new air-stable structure-simplified nafuredin-gamma analogs were designed and synthesized herein. Among all analogs synthesized, the one bearing a unique 1-azabicyclo[3.1.0] hexane scaffold showed the highest inhibitory activity (IC50 = 170 nM) while presenting high selectivity against nematode complex I.

机译：从天然Nafuredin获得的Nafuredin-Gamma已经证明了针对线虫复合物的有效和选择性的抑制活性I.然而，由于缀合的二烯是氧不稳定的，Nafuredin-γ在空气中不稳定。在没有共轭二烯的情况下，通过合成结构简化的Nafuredin-Gamma类似物自然解决了空气中的不稳定性。然而，这些改性的类似物显示出较低的我的抑制活动。因此，在本文中设计和合成了新的空气稳定结构简化的Nafuredin-Gamma类似物。在合成的所有类似物中，携带独特的1-氮杂双环[3.1.0]己烷支架的一个抑制活性（IC50 = 170nm），同时呈现对线虫复合物的高选择性I.

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来源
《The Journal of Antibiotics: An International Journal》 |2017年第5期|共8页
作者
Ohtawa Masaki; Arima Shiho; Shimizu Risa; Hanatani Naomi; Shimizu Eri; Shiomi Kazuro; Kita Kiyoshi; Omura Satoshi; Nagamitsu Tohru;
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作者单位

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Infect Control Sci Tokyo Japan;

Nagasaki Univ Sch Trop Med &

Global Hlth Nagasaki Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

Kitasato Univ Grad Sch Pharmaceut Sci Tokyo Japan;

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正文语种 eng
中图分类药学;
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1. Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor [J] . Ohtawa Masaki, Arima Shiho, Shimizu Risa, The Journal of Antibiotics: An International Journal . 2017,第5期

机译：开发新的空气稳定结构简化的Nafuredin-Gamma模拟，作为有效和选择性线性复合物I抑制剂
2. Changing the selectivity profile - from substrate analog inhibitors of thrombin and factor Xa to potent matriptase inhibitors [J] . Maiwald Alexander, Hammami Maya, Wagner Sebastian, Journal of enzyme inhibition and medicinal chemistry. . 2016,第Suppla1期

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Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor

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