期刊论文

Liu, Hao-Ran;Yan, Jian-Ye

英文

Molecular Diversity

1381-1991

2018

22

4

893-906

10.1007/s11030-018-9839-y

Natural science foundation of Hu'nan ProvinceNatural Science Foundation of Hunan Province [2017JJ2050, 2018JJ3572]; United States Public Health Service (NIH)United States Public Health ServiceUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USA [GM065307]; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USANIH National Institute of General Medical Sciences (NIGMS) [R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307, R01GM065307] Funding Source: NIH RePORTER

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Chalcones containing tertiary amine side-chains have potent activity as acetylcholinesterase (AChE) inhibitors. However, the effects of the location of the tertiary amine groups as well as of other groups on AChE and butyrylcholinesterase (BChE) activity have not been reported. Here, we report the synthesis and testing of 36 new coumarin-chalcone hybrids (5d-7j, 9d-11f, 12k-13m) against AChE and BChE. The nature and position of the chalcone substituents had major effects on inhibitory activity as well as selectivity for AChE over BChE. Compounds with para-substituted chalcone fragments in whic...