期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 1, 页码 1-10出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.054
关键词
Alzheimer's disease; Dihydroquinoline-3-carboxamides; Dihydroquinoline-3-carbohydrazides; hexahydropyrimido[5,4-c]quinoline-2,5-diones; AChE; BuChE; Molecular modeling; Ca channel antagonism
资金
- Conseil Regional de Franche-Comte
- Ministerio de Educacion y Ciencia [SAF 2007-65181]
The synthesis, biological evaluation, and molecular modeling of new 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides(4), 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbohydrazide (6), and some hexahydropyrimido[5,4-c]quinoline-2,5-diones (9) produced earlier by our laboratory, as AChE/BuChE inhibitors, is described. From these analyses compound 4c resulted equipotent regarding the inhibition of cholinesterases'; inhibitors 6k, 9a, 9b were selective for AChE, whereas product 4d proved selective for BuChE. Docking analysis has been carry out in order to identify the binding mode in the active site, and to explain the observed selectivities. Only compound 9a has been shown to decrease K+-induced calcium signals in bovine chromaffin cells. (C) 2010 Elsevier Masson SAS. All rights reserved.
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