title: New derivatives of 3,4-dihydroisoquinoline-3-carboxylic acid with free-radical scavenging, D-amino acid oxidase, acetylcholinesterase and butyrylcholinesterase inhibitory activity.
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.
authors.affiliation: National Institute of Public Health-National Institute of Hygiene, Chocimska 24, Warsaw 00-791, Poland. jsolecka@pzh.gov.pl.
authors.forename: Jolanta
authors.initials: J
authors.lastname: Solecka
authors.affiliation: National Institute of Public Health-National Institute of Hygiene, Chocimska 24, Warsaw 00-791, Poland. aguspiel@pzh.gov.pl.
authors.forename: Adam
authors.initials: A
authors.lastname: Guśpiel
authors.affiliation: National Institute of Public Health-National Institute of Hygiene, Chocimska 24, Warsaw 00-791, Poland. mpostek@pzh.gov.pl.
authors.forename: Magdalena
authors.initials: M
authors.lastname: Postek
authors.affiliation: National Institute of Public Health-National Institute of Hygiene, Chocimska 24, Warsaw 00-791, Poland. jziemska@pzh.gov.pl.
authors.forename: Joanna
authors.initials: J
authors.lastname: Ziemska
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. rkaw@uph.edu.pl.
authors.forename: Robert
authors.initials: R
authors.lastname: Kawęcki
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. katarzyna.leczycka@icho.edu.pl.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Lęczycka
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. agnieszka.osior@icho.edu.pl.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Osior
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. bartlomiej.pietrzak@gmail.com.
authors.forename: Bartłomiej
authors.initials: B
authors.lastname: Pietrzak
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. pypowski@uph.edu.pl.
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Pypowski
authors.affiliation: Institute of Chemistry, Siedlce University, 3.Maja 54, Siedlce 80-110, Poland. agatawyrzykowska@gmail.com.
authors.forename: Agata
authors.initials: A
authors.lastname: Wyrzykowska
mesh_terms: D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D003605:D-Amino-Acid Oxidase / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D016166:Free Radical Scavengers; C109852:G 1616; D007546:Isoquinolines; D003605:D-Amino-Acid Oxidase; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase