New Derivatives of 3,4-Dihydroisoquinoline-3-carboxylic Acid with Free-Radical Scavenging, D-Amino Acid Oxidase, Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activity

作者：Solecka Jolanta^*; Guspiel Adam; Postek Magdalena; Ziemska Joanna; Kawecki Robert; Leczycka Katarzyna; Osior Agnieszka; Pietrzak Bartlomiej; Pypowski Krzysztof; Wyrzykowska Agata

来源：Molecules, 2014, 19(10): 15866-15890.

DOI：10.3390/molecules191015866

• free radicals
• scavenger
• DAAO
• AChE
• BuChE
• inhibitor
• 3,4-dihydroisoquinoline

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 center dot), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical (ABTS(center dot+)), superoxide anion radical (O-2(center dot+)) 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.

• 出版日期2014-10