期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 97, 期 -, 页码 181-189出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.04.055
关键词
Acetylcholinesterase; Alzheimer's disease; Chroman-4-one; Docking study; Homoisoflavonoids
资金
- Research Council of Tehran University of Medical Sciences
- Iran National Science Foundation (INSF)
A series of 3-(4-(aminoalkoxy)benzylidene)-chroman-4-ones 7a-r were designed and synthesized as analogs of homoisoflavonoids which are well known natural products with diverse pharmacological properties related to Alzheimer's disease. The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE and BuChE, revealed that compounds bearing piperidinylethoxy residue showed potent activity against AChE at sub-micromolar level (IC50 values = 0.122-0.207 mu M), more potent than reference drug tacrine. The structure-activity relationships study of piperidinylethoxy series demonstrated that the selectivity and physicochemical properties of compounds could be optimized by selection of a proper substituent on the C-7 position of chroman ring, while the high potency of the molecule against AChE was reserved. (C) 2015 Elsevier Masson SAS. All rights reserved.
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