carboxamide Derivatives, Multi-Target Inhibitors of Monoamine Oxidase and Cholinesterase: Design, Synthesis, and Biological Activity

A series of (S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives was synthesized and evaluated for inhibitory activity against monoamine oxidase (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). Four compounds (2i, 2p, 2t, and 2v) showed good inhibitory...

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Published inMolecules (Basel, Switzerland) Vol. 28; no. 4
Main Authors Jin, Qing-Hao, Zhang, Li-Ping, Zhang, Shan-Shan, Zhuang, Dai-Na, Zhang, Chu-Yu, Zheng, Zhou-Jun, Guan, Li-Ping
Format Journal Article
LanguageEnglish
Published MDPI AG 01.02.2023
Subjects
Acetylcholine
Advertising executives
Alzheimer's disease
Depression, Mental
Nervous system diseases
Oxidases
Resveratrol
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Summary:A series of (S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives was synthesized and evaluated for inhibitory activity against monoamine oxidase (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). Four compounds (2i, 2p, 2t, and 2v) showed good inhibitory activity against both MAO-A and MAO-B, and two compounds (2d and 2j) showed selective inhibitory activity against MAO-A, with IC[sub.50] values of 1.38 and 2.48 µM, respectively. None of the compounds showed inhibitory activity against AChE; however, 12 compounds showed inhibitory activity against BChE. None of the active compounds showed cytotoxicity against L929cells. Molecular docking revealed several important interactions between the active analogs and amino acid residues of the protein receptors. This research paves the way for further study aimed at designing MAO and ChE inhibitors for the treatment of depression and neurodegenerative disorders.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules28041654