Synthesis of 1,5-Anhydro-d-fructose derivatives and evaluation of their inflammasome inhibitors

Autor: Junko Amano, Kohtaro Goto, Hiroko Ideo, Takashi Shirai, Satoshi Noma, Akio Matsuda, Ikuro Maruyama, Akiko Tsuchida, Yuriko Hirose, Mamoru Mizuno
Rok vydání: 2017
Předmět:
Zdroj: Bioorganicmedicinal chemistry. 26(13)
ISSN: 1464-3391
Popis: Synthesis of several 1,5-Anhydro-d-fructose (1,5-AF) derivatives to evaluate inhibitory activities of the inflammasome was carried out. Recently, 1,5-AF reported to suppress the inflammasome, although with only low activity. We focused on the hydration of 2-keto form of 1,5-AF and speculated that this hydration was the cause of low activity. Therefore, we synthesized some 1,5-AF derivatives that would not be able to form the dimer conformation and can be expected to have high activity against inflammasome, and then evaluated their inhibitory activities with respect to the NLRP3 inflammasome by using mouse bone marrow-derived macrophages and human THP-1 cells. As a result, some synthesized 2-keto form compounds had much higher inhibitory activities with respect to the NLRP3 inflammasome than did 1,5-AF.
Databáze: OpenAIRE