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Review Article

抗胆碱酯酶药物治疗阿尔茨海默病:最新综述

卷 30, 期 6, 2023

发表于: 07 October, 2022

页: [701 - 724] 页: 24

弟呕挨: 10.2174/0929867329666220803113411

价格: $65

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摘要

背景:阿尔茨海默病(AD)是一种进行性神经退行性疾病，损害认知系统并导致痴呆。一般来说，AD影响65岁以上的人，如果我们考虑到预期寿命的增加，这意味着社会影响。目前市场上的药物只能减缓疾病的发展。从这个意义上说，寻找新药是药物化学的一个相关课题。本研究采用的治疗策略为胆碱能假说，其中乙酰胆碱酯酶(AChE)抑制剂是本病的主要治疗方法。 目的:综述具有AChE抑制功能的合成化合物和天然化合物的研究进展。 方法:根据2010年最后5年AChE抑制剂的研究收集数据。对合成和天然化合物进行了研究，其中采用了配体药物设计(LBDD)和结构药物设计(SBDD)策略，以更好地了解有前景的治疗药物的构效关系。 结果:用于计算生物利用度雷达、亲脂性、类药性和药代动力学参数的物理化学和药代动力学性质的预测(SwissADME)表明，大多数活性化合物与以下特征相关:分子量大于377 g/mol;摩尔折射率大于114;分数Csp3小于0.39,TPSA大于43 Å2。大多数活性化合物的亲脂性参数在2.5 ~ 4.52之间，具有主要的亲脂性特征。研究了与药物开发相关的原子和键/相互作用，数据指出了以下趋势:重原子数在16 ~ 41之间;芳香族重原子数在6 ~ 22之间;1 ~ 14之间的可旋转键数;h -键受体数量在1 ~ 11之间;h -债券捐赠者少于7个。分子对接研究表明，所有化合物的goldscore都高于作为阳性对照的药物，表明与酶的相互作用更强。 结论:所选化合物具有开发新型抗胆碱酯酶药物的潜力，可作为开发新候选药物的良好起点。此外，设计规则也可以从我们的分析中提取出来。

关键词: 阿尔茨海默病 (AD)、AChE 抑制剂、分子对接、构效关系 (SAR)、基于结构的药物设计 (SBDD)、基于配体的药物设计 (LBDD)、药代动力学。

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