Knez Damijan, Sova Matej, Košak Urban, Gobec Stanislav
Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
Future Med Chem. 2017 May;9(8):811-832. doi: 10.4155/fmc-2017-0036. Epub 2017 May 15.
Accumulating evidence indicates a solid relationship between several enzymes and Alzheimer's disease. Cholinesterases and monoamine oxidases are closely associated with the disease symptomatology and progression and have been tackled simultaneously using several multifunctional ligands. This design strategy offers great chances to alter the course of Alzheimer's disease, in addition to alleviation of the symptoms. More than 15 years of research has led to the identification of various dual cholinesterase/monoamine oxidase inhibitors, while some showing positive outcomes in clinical trials, thus giving rise to additional research efforts in the field. The aim of this review is to provide an update on the novel dual inhibitors identified recently and to shed light on their therapeutic potential.
越来越多的证据表明，几种酶与阿尔茨海默病之间存在紧密联系。胆碱酯酶和单胺氧化酶与该疾病的症状学及进展密切相关，并且已经通过多种多功能配体同时对它们进行研究。这种设计策略除了能缓解症状外，还为改变阿尔茨海默病的病程提供了巨大机会。超过15年的研究已导致多种双胆碱酯酶/单胺氧化酶抑制剂被鉴定出来，其中一些在临床试验中显示出积极结果，从而引发了该领域更多的研究工作。本综述的目的是提供关于最近鉴定出的新型双抑制剂的最新信息，并阐明它们的治疗潜力。
