25015-92-3Relevant articles and documents
Design, synthesis and evaluation of novel 4-dimethylamine flavonoid derivatives as potential multi-functional anti-Alzheimer agents
Luo, Wen,Su, Ya-Bin,Hong, Chen,Tian, Run-Guo,Su, Lei-Peng,Wang, Yue-Qiao,Li, Yang,Yue, Jun-Jie,Wang, Chao-Jie
, p. 7275 - 7282 (2013)
A series of 4-dimethylamine flavonoid derivatives 5a-5r were designed, synthesized and evaluated as potential multi-functional anti-Alzheimer agents. The results showed that most of the synthesized compounds exhibited high acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at the micromolar range (IC50, 1.83-33.20 μM for AChE and 0.82-11.45 μM for BChE). A Lineweaver-Burk plot indicated a mixed-type inhibition for compound 5j with AChE, and molecular modeling study showed that 5j targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE. Besides, the derivatives showed potent self-induced Aβ aggregation inhibitory activity at 20 μM with percentage from 25% to 48%. In addition, some compounds (5j-5q) showed potent oxygen radical absorbance capacity (ORAC) ranging from 1.5- to 2.6-fold of the Trolox value. These compounds should be further investigated as multi-potent agents for the treatment of Alzheimer's disease.
Design and biological evaluation of novel imidazolyl flavonoids as potent and selective protein tyrosine phosphatase inhibitors
Ge, Yu,Han, Rong Y.,Wang, Qing M.,Zhang, Ling
, p. 563 - 574 (2020/06/21)
Background: Protein tyrosine phosphatases 1B are considered to be a desirable vali-dated target for therapeutic development of type II diabetes and obesity. Methods: A new series of imidazolyl flavonoids as potential protein tyrosine phosphatase inhibi-to
Tryptophan compound, preparation method and application thereof
-
Paragraph 0030-0037; 0050-0052; 0058-0060, (2019/11/28)
The invention relates to a tryptophan compound, a preparation method and application thereof. The molecular formula is (Z)-(2-((2-(4-methoxybenzylidene)-3-oxo-2, 3-dihydrobenzofuran-6-yl)oxyl)acetyl)-D-tryptophan. The small molecule compound has a chiral center, and the absolute configuration is R configuration; the small molecule compound can reach a good inhibitory effect on thrombin, also has low toxicity, good druggability, and good medicinal potential, and provides a new potential option for clinical medication.