Synthesis, characterization, crystal structure and biological evaluation of 1,3,5-triazine-quinoline derivatives as butyrylcholinesterase inhibitors

被引：6

作者：

Su, Jia-bin ^{[1
,2
]}

Wu, Wen-long ^{[2
]}

Dong, Chang-E ^{[2
]}

Yang, Shun ^{[2
]}

Feng, Yuan-yuan ^{[2
]}

Qin, Tian ^{[2
]}

Chen, Ke-qi ^{[2
]}

Qian, Jing-jing ^{[2
]}

Zou, Jing-pei ^{[2
]}

Liu, Yu-Han ^{[2
]}

Liu, Shan-ming ^{[2
]}

Liu, Wei-Wei ^{[3
]}

Shi, Da-Hua ^{[1
,2
]}

机构：

[1] Jiangsu Ocean Univ, Jiangsu Key Lab Marine Biotechnol, Jiangsu Key Lab Marine Bioresources & Environm, Lianyungang 222005, Peoples R China

[2] Jiangsu Ocean Univ, Sch Pharm, Lianyungang 222005, Peoples R China

[3] Coinnovat Ctr Jiangsu Marine Bioind Technol, Lianyungang 222005, Peoples R China

来源：

JOURNAL OF MOLECULAR STRUCTURE | 2023年 / 1274卷

关键词：

Cholinesterase inhibitory activity; Quinoline derivatives; 13; 5-triazine derivatives; TRIAZINE; CHOLINESTERASES; QUINOLINE; HYBRIDS; DESIGN;

D O I：

10.1016/j.molstruc.2022.134391

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

Sixteen new 1,3,5-triazine-quinoline derivatives were designed and synthesized and evaluated as cholinesterase inhibitors. The structure of 1,3,5-triazine-quinoline derivatives were confirmed by IR, NMR, HRMS and single crystal X-ray diffraction experiments. Compound 5j had a monoclinic crystal sys-tem and P21/c space group. Compound 5k had a monoclinic crystal system and C2/c space group. The cholinesterase inhibitory activity of the synthetic compounds were measured using the colorimetric Ell-man's method. Compound 5 g showed best acetylcholinesterase inhibitory activity with IC50 value of 10.82 mu M and butyrylcholinesterase inhibitory activity with IC50 value of 0.046 mu M. Molecular docking showed that the compound 5 g could interacted with the active site of butyrylcholinesterase.(c) 2022 Elsevier B.V. All rights reserved.

引用

页数：10

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