143033-86-7Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of a new series of biphenyl/bibenzyl derivatives functioning as dual inhibitors of acetylcholinesterase and butyrylcholinesterase
Wang, Dong-Mei,Feng, Bo,Fu, Hui,Liu, Ai-Lin,Wang, Lin,Du, Guan-Hua,Wu, Song
, (2017)
Alzheimer's disease (AD), the most common form of dementia in adults, is a progressive neurodegenerative disorder of the brain characterized by loss of memory and steady deterioration of cognition. Here, a series of symmetrical molecules containing biphenyl/bibenzyl scaffolds (12-36) were designed, synthesized, and evaluated for their ability to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A biological evaluation showed that most of these biphenyl derivatives were potent AChE and BuChE inhibitors. Among them, compound 15 displayed the greatest ability to inhibit BuChE (IC50 = 0.74 μM) and was also a good AChE inhibitor (IC50 = 1.18 μM). Compound 19 was not only a potent AChE inhibitor (IC50 = 0.096 μM), but also a mild BuChE inhibitor (IC50 =1.25 μM). Overall, these results suggested that compound 19 may be a promising agent in the treatment of AD.
SYNTHESIS OF 1--2-PHENYLETHANEDIONE
Lukac, Ivan,Mohapatra, Gour K. Das
, p. 1085 - 1091 (2007/10/02)
1--2-phenylethanedione (I) was prepared by Friedel-Crafts acylation of (3-chloropropyl)benzene with phenylacetyl chloride, oxidation with SeO2 of the resulting 1--2-phenyl-1-ethanone (IV) to 1-4-(3-c
