13290-31-8Relevant articles and documents
Thioether-bridged arylalkyl-linked N-phenylpyrazole derivatives: Design, synthesis, insecticidal activities, structure-activity relationship and molecular-modeling studies
Fei, Chengcheng,Chen, Yanfei,Jiang, Zhiyan,Jiang, Dingxin
, p. 1792 - 1796 (2018)
Owing to thioether diverse physicochemical properties by non-covalent interactions with bio-macromolecules, thioether derivatives containing heterocyclic moiety are known for their interesting insecticidal bioactivities and attracting considerable attenti
PYRIMIDINE OR PYRIDOPYRIDONE COMPOUND AND APPLICATION THEREOF
-
Paragraph 0046; 0060, (2018/11/21)
The present invention discloses a pyrimidine or pyridopyridone compound as shown in formula (I) and an application thereof relating to the technical field of medicament preparation. The compound can selectively suppress cyclin-dependent kinases (Cdks) CDK
Synthesis and biological evaluation of berberine-thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aβ aggregation and antioxidant activity
Su, Tao,Xie, Shishun,Wei, Hui,Yan, Jun,Huang, Ling,Li, Xingshu
, p. 5830 - 5840 (2013/09/12)
A series of berberine-thiophenyl hybrids were designed, synthesised, and evaluated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and β-amyloid (Aβ) aggregation and as antioxidants. Among these hybrids, compounds 4f and 4i, berberine linked with o-methylthiophenyl and o-chlorothiophenyl by a 2-carbon spacer, were observed to be potent inhibitors of AChE, with IC50 values of 0.077 and 0.042 μM, respectively. Of the tested compounds, 4i was also the most potent inhibitor of BuChE, with an IC50 value of 0.662 μM. Kinetic studies and molecular modelling simulations of the AChE-inhibitor complex indicated that a mixed-competitive binding mode existed for these berberine derivatives. The biological studies also demonstrated that these hybrids displayed interesting activities, including Aβ aggregation inhibition and antioxidant properties.