Structure–activity relationship study of the anti‐obesity natural product yoshinone A
作者:Yoshinori Kawazoe、Yuki Itakura、Toshiyasu Inuzuka、Sachikazu Omura、Daisuke Uemura
DOI:10.1002/chir.23292
日期:2021.5
to inhibit adipogenic differentiation. The natural compound is composed of a γ‐pyrone ring and a side chain and that contains two asymmetric carbons. Although their absolute configuration has been determined, there is no information available on the stereoisomers and their bioactivities. To address this question, we synthesized all four stereoisomers and measured their activities. We also prepared three
Yoshinone A 源自海藻,可抑制脂肪形成分化。该天然化合物由 γ-吡喃酮环和侧链组成,并含有两个不对称碳。尽管它们的绝对构型已确定,但没有关于立体异构体及其生物活性的信息。为了解决这个问题,我们合成了所有四种立体异构体并测量了它们的活性。我们还制备了另外三种 yoshinone A 衍生物,发现侧链内部的立体构型、γ-吡喃酮环和侧链的体积都在其活性中发挥着重要作用。我们的研究结果应有助于阐明 yoshinone A 的作用机制。