27891-44-7Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of carbamate derivatives of N-salicyloyl tryptamine as multifunctional agents for the treatment of Alzheimer's disease
Liu, Dan,Zhang, Honghua,Wang, Yuying,Liu, Wencheng,Yin, Gaofeng,Wang, Degui,Li, Junfang,Shi, Tao,Wang, Zhen
, (2021/12/20)
In this study, we designed, synthesized, and evaluated a series of carbamate derivatives of N-salicyloyl tryptamine as multifunctional therapeutic agents for the treatment of Alzheimer's disease (AD). After screening the acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitory activities, target compound 1g stood out as a mixed type reversible dual inhibitor of AChE and BChE. In addition, molecular docking studies were conducted to explore the actions on AChE and BChE. The results showed that 1g could decrease the level of pro-inflammatory cytokines NO, iNOS, IL-6, TNF-α, and ROS, increase the level of anti-inflammatory cytokines IL-4, and inhibit the aggregation of Aβ1-42. Moreover, the administration of 1g suppressed the activity of AChE in the brain. In a word, the compound 1g is effective for improving learning and memory behavior, blood-brain barrier permeation, pharmacokinetics, ChE inhibition, and anti-neuroinflammation. It may be considered as a promising multi-functional therapeutic agent for further investigation for the treatment of AD.
Benzoic acid tryptamine derivative as well as preparation method and application thereof
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Paragraph 0033-0034, (2021/10/30)
The invention provides a benzoic acid tryptamine derivative as well as preparation and application thereof. The benzoic acid tryptamine derivative uses a salicylic acid compound as a starting raw material and is protected by benzyl. The method comprises the following four-step reaction synthesis of carbamylation, deprotection and condensation. The benzoic acid tryptamine derivative prepared by the invention has dual inhibition effects of acetylcholinesterase and butyrylcholine esterase. Moreover, as a hybrid reversible inhibitor, the content and expression AChE of cells and animals can be reduced. , Good anti-neuroinflammation activity can be achieved, A β aggregation can be inhibited, BACE-1 expression is reduced. The learning memory and anti-depression ability of AD model mice can be remarkably improved, no obvious toxicity exists on cells and animals, and the drug has good pharmacokinetic performance and blood brain barrier permeability, and can be applied to preparation of's disease treatment drugs.
