d-葡萄糖共轭苯并噻唑-噻唑烷-4-酮杂化物：作为多靶点抗阿尔茨海默病化合物的设计与合成
d‑Glucose-Conjugated Benzo[]thiazole-thiazolidin-4-one Hybrids: Design and Synthesis as Multitarget Anti-Alzheimer Compounds.
作者信息
Thanh Nguyen Dinh, Toan Vu Ngoc, Hai Do Son, Tri Nguyen Minh, Toan Duong Ngoc, Trang Vu Minh
机构信息
Faculty of Chemistry, VNU University of Science (Vietnam National University, Ha Noi), 19 Le Thanh Tong, Hoan Kiem, Ha Noi 10000, Viet Nam.
Institute of Science and Technology, Ministry of Public Security of Vietnam, 47 Pham Van Dong, Cau Giay, Ha Noi 10000, Viet Nam.
出版信息
ACS Med Chem Lett. 2025 May 5;16(6):1024-1030. doi: 10.1021/acsmedchemlett.5c00064. eCollection 2025 Jun 12.
A new series of d-glucose-conjugated 2,3-thiazoline-benzo-[]-thiazole hybrid compounds - were synthesized from reaction of the corresponding thioureas - and ethyl bromoacetate in the presence of sodium acetate in chloroform. The evaluations for anti-Alzheimer activity showed that some compounds exhibited remarkable inhibitory activity against AChE and BChE as well as against MAO-A and MAO-B enzymes. The orders of inhibition for each enzyme of these compounds were as follows: > (against AChE), > (against BChE), > > (against MAO-A), and > (against MAO-B). Compound was an inhibitor of interest due to its potent or good activity against the two studied enzymes BChE and MAO-B, respectively. Compounds (against AChE) and (against (BChE) had a competitive type with constants of 16.93 and 17.09 nM, respectively. The most potential compounds , , and were not cytotoxic on 3T3 cells and had high levels of safety.
一系列新的d-葡萄糖共轭的2,3-噻唑啉-苯并[]-噻唑杂化化合物——由相应的硫脲与溴乙酸乙酯在醋酸钠存在下于氯仿中反应合成。抗阿尔茨海默病活性评估表明，一些化合物对乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）以及单胺氧化酶A（MAO-A）和单胺氧化酶B（MAO-B）均表现出显著的抑制活性。这些化合物对每种酶的抑制顺序如下： ＞ （针对AChE）， ＞ （针对BChE）， ＞ ＞ （针对MAO-A），以及 ＞ （针对MAO-B）。化合物 因其分别对所研究的两种酶BChE和MAO-B具有强效或良好活性而成为有意义的抑制剂。化合物 （针对AChE）和 （针对BChE）具有竞争类型，其 常数分别为16.93和17.09 nM。最具潜力的化合物 、 和 对3T3细胞无细胞毒性且具有高安全性。
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