基于自然特权支架的单氨酸氧化酶B抑制剂:系统结构修饰的综述
Yangjing Lv1, Zhiyuan Zheng1, Renzheng Liu1
1College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China.
自然产品为开发选择性单胺氧化酶B (MAO-B) 抑制剂提供了有前途的支架. 这篇评论探讨了它们的结构-活性关系,用于治疗像帕金森氏症和阿尔茨海默氏症这样的神经退行性疾病.
科学领域:
- 生物化学 生物化学
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 单胺氧化酶 (MAO) 酶,特别是MAO-B,在神经递质代谢中至关重要.
- 由于MAO-B活性和副产品的氧化应激会导致神经退行性疾病 (NDs).
- 抑制MAO-B是对帕金森病 (PD) 和阿尔茨海默病 (AD) 等ND的治疗点.
研究的目的:
- 审查来自自然支架的MAO-B抑制剂的结构活性关系 (SAR).
- 突出自然产品在发现新型MAO-B抑制剂方面的潜力.
- 讨论基于天然支架的MAO-B抑制剂的优点和局限性.
主要方法:
- 在过去的20年中,文学综述专注于MAO-B抑制剂和天然产品.
- 对特权自然支架的结构-活动关系 (SAR) 的分析.
- 合成和评估天然产品衍生物作为MAO-B抑制剂.
主要成果:
- 天然支架,如染色体,素,,咖啡因和光子是MAO-B抑制剂设计的特权结构.
- 对于这些支架存在重要的SAR数据,指导抑制剂的开发.
- 很少有来自自然来源的选择性和可逆MAO-B抑制剂获得临床批准.
结论:
- 自然产品为开发有效的MAO-B抑制剂提供了丰富的来源.
- 对基于天然支架的MAO-B抑制剂的进一步研究对于ND治疗是有必要的.
- 对这一领域的挑战和机遇有一个平衡的视角对于未来的药物开发至关重要.
更多相关视频
08:12Surface Functionalization of Metal-Organic Frameworks for Improved Moisture Resistance
Published on: September 5, 2018
10:17Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
相关概念视频
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Drugs Affecting Neurotransmitter Synthesis
Adrenergic Agonists: Indirect-Acting Agents
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Antidepressant Drugs: MAOIs and Other Agents
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline...
