65117-29-5Relevant articles and documents
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.
BENZOIC ACID COMPOUNDS AND USE THEREOF AS MEDICAMENTS
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, (2008/06/13)
Benzoic acid compounds of the formula STR1 wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.
DIRECT CONVERSION OF CARBOXYLIC ACIDS AND CARBOXYLIC ESTERS INTO S,S'-DIPHENYL ACETALS AND PHENYL SULFIDES WITH THEXYLPHENYLTHIOBORANE
Kim, Sunggak,Kim, Sung Soo
, p. 1913 - 1916 (2007/10/02)
Reaction of carboxylic acids with thexylphenylthioborane in methylene chloride at room temperature gives S,S-diphenyl acetals in high yields and carboxylic esters are converted into phenyl sulfides in the presence of zinc iodide under similar conditions.