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Total synthesis of 4-epi-atpenin A5 as a potent nematode complex II inhibitor
Authors:Daiki Lee  Hiroki Kondo  Yui Kuwayama  Kento Takahashi  Shiho Arima  Satoshi Omura  Masaki Ohtawa  Tohru Nagamitsu
Institution:1. Department of Synthetic Natural Products Chemistry and Medicinal Research Laboratories, School of Pharmacy, Kitasato University, 5–9–1 Shirokane, Minato-ku, Tokyo 108–8641, Japan;2. Kitasato Institute for Life Sciences, Kitasato University, Tokyo 108-8641, Japan
Abstract:It is clear that atpenins and their analogs are useful chemical tools for elucidation of complex II functionality and that they could act as lead compounds for the development of novel helminth complex II-specific inhibitors. Recently, we discovered 4-epi-atpenin A5 as a potent nematode complex II inhibitor during our SAR studies of atpenin A5. This result led us to embark on a concise total synthesis of 4-epi-atpenin A5. In this study, we describe the total synthesis of 4-epi-atpenin A5. Importantly, this was more concise and practical synthesis than our previous total synthesis of atpenin A5.
Keywords:Corresponding author    Atpenin A5  Nematode complex II inhibitor  Total synthesis
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