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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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Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor
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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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Journal Article
Development of a new air-stable structure-simplified nafuredin-gamma analog as a potent and selective nematode complex I inhibitor
2017
Overview
Nafuredin-γ, obtained from natural nafuredin, has demonstrated a potent and selective inhibitory activity against nematode complex I. However, nafuredin-γ 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-γ analogs without conjugated dienes. However, these modified analogs showed lower complex I inhibitory activities. Therefore, new air-stable structure-simplified nafuredin-γ 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 (IC 50 =170 nM) while presenting high selectivity against nematode complex I.
Publisher
Nature Publishing Group
Subject
