Synthesis of cynaropicrin-d₄

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• 作者：Takuya Sato^a ; Shihori Hara^a ; Makiko Sato^a ; Keita Ogawa^a ; Michael Adams^b ; Toyonobu Usuki^a ; ^{t-usuki@sophia.ac.jp" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Cynaropicrin ; Guaianolide ; Trypanosoma brucei ; Pharmacokinetic study ; Deuterium
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：1 December 2015
• 年：2015
• 卷：25
• 期：23
• 页码：5504-5507
• 全文大小：474 K

文摘

Cynaropicrin is a guaianolide sesquiterpene lactone, which has potent in vitro and in vivo inhibitory activity against Trypanosoma brucei, the protozoan parasite that causes human African trypanosomiasis (HAT; sleeping sickness). Herein, we describe the synthesis of cynaropicrin’s deuterated derivative, cynaropicrin-d₄, by the replacement of the side chain of natural cynaropicrin. The synthesized cynaropicrin-d₄ could be employed as an internal standard for liquid chromatography–mass spectrometry (LC–MS) analysis, in the pharmacokinetic study of cynaropicrin. This could potentially advance the study of this therapeutic lead.