3044-57-3Relevant academic research and scientific papers
Inhibitory effect of flavonoids on human glutaminyl cyclase
Li, Manman,Dong, Yao,Yu, Xi,Zou, Yongdong,Zheng, Yizhi,Bu, Xianzhang,Quan, Junmin,He, Zhendan,Wu, Haiqiang
, p. 2280 - 2286 (2016/04/26)
Glutaminyl cyclase (QC) plays an important role in the pathogenesis of Alzheimer's disease (AD) and can be a potential target for the development of novel anti-AD agents. However, the study of QC inhibitors are still less. Here, phenol-4′ (R1-), C5-OH (R2-) and C7-OH (R3-) modified apigenin derivatives were synthesized as a new class of human QC (hQC) inhibitors. The efficacy investigation of these compounds was performed by spectrophotometric assessment and the structure-activity relationship (SAR) was evaluated. Molecular docking was also carried out to analyze the binding mode of the synthesized flavonoid to the active site of hQC.
Regioselective synthesis of flavone derivatives via DMAP-catalyzed cyclization of o-alkynoylphenols
Yoshida, Masahito,Fujino, Yuta,Saito, Koya,Doi, Takayuki
experimental part, p. 9993 - 9997 (2012/02/06)
A catalytic amount of DMAP promoted cyclization of o-alkynoylphenols via a 6-endo cyclization mode leading to flavone derivatives in high yields without forming 5-exo cyclized aurone derivatives. Utilizing this method, methoxy substituted flavone and alkyl substituted γ-benzopyranone derivatives were synthesized.
Synthesis of γ-benzopyranone by TfOH-promoted regioselective cyclization of o-alkynoylphenols
Yoshida, Masahito,Fujino, Yuta,Doi, Takayuki
supporting information; experimental part, p. 4526 - 4529 (2011/10/09)
Regioselective cyclization of o-alkynoylphenols forming γ-benzopyranones has been demonstrated. Trifluoromethanesulfonic acid (TfOH) induced 6-endo cyclization of o-alkynoylphenols without forming 5-exo cyclized benzofuranone derivatives to provide the corresponding γ-benzopyranones in high yields.
