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基于多胺骨架的乙酰胆碱酯酶非共价抑制剂的构效关系。4. 对内部间隔基的进一步研究。

Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.

作者信息

Tumiatti Vincenzo, Milelli Andrea, Minarini Anna, Rosini Michela, Bolognesi Maria Laura, Micco Marialuisa, Andrisano Vincenza, Bartolini Manuela, Mancini Francesca, Recanatini Maurizio, Cavalli Andrea, Melchiorre Carlo

机构信息

Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.

出版信息

J Med Chem. 2008 Nov 27;51(22):7308-12. doi: 10.1021/jm8009684.

DOI:10.1021/jm8009684
PMID:18954037
Abstract

Novel multi-target-directed ligands were designed by replacing the inner dipiperidino function of 3 with less flexible or completely rigid moieties to obtain compounds endowed with multiple biological properties that might be relevant to Alzheimer's disease. 15 was the most interesting, inhibiting AChE in the nanomolar range and inhibiting AChE-induced and self-promoted beta-amyloid aggregation in the micromolar range.

摘要

通过用柔性较小或完全刚性的基团取代3的内部双哌啶功能，设计了新型多靶点导向配体，以获得具有多种可能与阿尔茨海默病相关生物学特性的化合物。15是最有趣的，它在纳摩尔范围内抑制乙酰胆碱酯酶，并在微摩尔范围内抑制乙酰胆碱酯酶诱导的和自我促进的β-淀粉样蛋白聚集。

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Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.基于多胺骨架的乙酰胆碱酯酶非共价抑制剂的构效关系。4. 对内部间隔基的进一步研究。
J Med Chem. 2008 Nov 27;51(22):7308-12. doi: 10.1021/jm8009684.
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