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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H-3 receptor ligands
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Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H-3 receptor ligands

机译：氯苯氧基衍生物-组胺H-3受体配体的胆碱酯酶抑制活性

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In recent years, multitarget-directed ligands have become an interesting strategy in a search for a new treatment of Alzheimer's disease. Combination of both: a histamine H-3 receptor antagonist/inverse agonist and a cholinesterases inhibitor in one molecule could provide a new therapeutic opportunity. Here, we present biological evaluation of histamine H-3 receptor ligands-chlorophenoxyalkylamine derivatives against cholinesterases: acetyl- and butyrylcholinesterase. The target compounds showed cholinesterase inhibitory activity in a low micromolar range. The most potent in this group was 1-(7-(4-chlorophenoxy) heptyl) homopiperidine (18) inhibiting the both enzymes (EeAChE IC50 = 1.93 mu M and EqBuChE IC50 = 1.64 mu M). Molecular modeling studies were performed to explain the binding mode of 18 with histamine H-3 receptor as well as with cholinesterases. (C) 2016 Published by Elsevier Ltd.
机译：近年来，在寻找新的阿尔茨海默氏病治疗方法中，多靶标定向配体已成为一种有趣的策略。组胺H-3受体拮抗剂/反向激动剂和胆碱酯酶抑制剂的组合可在一个分子中提供新的治疗机会。在这里，我们目前对胆碱酯酶：乙酰-和丁酰胆碱酯酶的组胺H-3受体配体-氯苯氧基烷基胺衍生物的生物学评估。目标化合物在低微摩尔范围内显示胆碱酯酶抑制活性。该组中最有效的是抑制两种酶的1-（7-（4-氯苯氧基）庚基）高哌啶（18）（EeAChE IC50 = 1.93μM和EqBuChE IC50 = 1.64μM）。进行分子建模研究以解释18与组胺H-3受体以及胆碱酯酶的结合模式。 （C）2016由Elsevier Ltd.出版

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