New derivatives of 3,4-dihydroisoquinoline-3-carboxylic acid with free-radical scavenging, D-amino acid oxidase, acetylcholinesterase and butyrylcholinesterase inhibitory activity

具有自由基清除、D-氨基酸氧化酶、乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性的3,4-二氢异喹啉-3-羧酸新衍生物

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作者:Jolanta Solecka, Adam Guśpiel, Magdalena Postek, Joanna Ziemska, Robert Kawęcki, Katarzyna Lęczycka, Agnieszka Osior, Bartłomiej Pietrzak, Krzysztof Pypowski, Agata Wyrzykowska

Abstract

A series of 3,4-dihydroisoquinoline-3-carboxylic acid derivatives were synthesised and tested for their free-radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH·), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical (ABTS·+), superoxide anion radical (O2·-) and nitric oxide radical (·NO) assays. We also studied d-amino acid oxidase (DAAO), acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. Almost each of newly synthesised compounds exhibited radical scavenging capabilities. Moreover, several compounds showed moderate inhibitory activities against DAAO, AChE and BuChE. Compounds with significant free-radical scavenging activity may be potential candidates for therapeutics used in oxidative-stress-related diseases.

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