期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 11, 页码 1325-1329出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.03.050
关键词
Acetylcholinesterase inhibitors; Butyrylcholinesterase inhibitors; Alzheimer's disease; 4-N-phenylaminoquinoline; Molecular modeling
资金
- Training Project of Innovation Team of Colleges and Universities in Tianjin [TD13-5020]
Dual binding site acetylcholinesterase (AChE) inhibitors and butyrylcholinesterase (BChE) inhibitors have recently emerged as two classes of new anti-Alzheimer agents to positively modify the disease's course. In this work, a new series of 4-N-phenylaminoquinolines was synthesized and evaluated for their abilities to inhibit AChE and BChE. Compound 11b showed significant inhibitory activities on AChE and BChE with IC50 values of 0.86 and 2.65 mu M, respectively, a lot better than that of reference drug galanthamine. Furthermore, docking study showed that compound 11b interacted simultaneously not only with active and peripheral sites of AChE, but also with all five regions of BChE active site. These findings suggest that these derivatives could be regarded as promising starting points for further drug discovery developments.
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