Synthesis and biological evaluation of benzochromenopyrimidinones as cholinesterase inhibitors and potent antioxidant, non-hepatotoxic agents for Alzheimer's disease

Dgachi, Youssef (author), Bautista-Aguilera, Oscar M. (author), Benchekroun, Mohamed (author), Martin, Hélène (author), Bonet, Alexandre (author), Knez, Damijan (author), Godyń, Justyna (author), Malawska, Barbara (author), Gobec, Stanislav (author), Chioua, Mourad (author), Janockova, Jana (author), Soukup, Ondrej (author), Chabchoub, Fakher (author), Marco-Contelles, José (author), Ismaili, Lhassane (author)

We report herein the straightforward two-step synthesis and biological assessment of novel racemic benzochromenopyrimidinones as non-hepatotoxic, acetylcholinesterase inhibitors with antioxidative properties. Among them, compound 3Bb displayed a mixed-type inhibition of human acetylcholinesterase (IC$_{50}$ = 1.28 % 0.03 µM), good antioxidant activity, and also proved to be non-hepatotoxic on human HepG2 cell line.

• Language: English
• Keywords: Alzheimer's disease, quinazolinones, multicomponent reactions, multitarget-directed ligands, antioxidants, cholinesterase inhibitors, hepatotoxicity
• Work type: Article
• Typology: 1.01 - Original Scientific Article
• Organization: FFA - Faculty of Pharmacy
• Publication status: Published
• Publication version: Version of Record
• Year: 2016
• Number of pages: 15 str.
• Numbering: Vol. 21, iss. 5, art. 634
• PID: 20.500.12556/RUL-130298
• UDC: 615.2:616.894
• ISSN on article: 1420-3049
• DOI: 10.3390/molecules21050634
• COBISS.SI-ID: 4083825
• Publication date in RUL: 13.09.2021

Record is a part of a journal

• Title: Molecules
• Shortened title: Molecules
• Publisher: MDPI
• ISSN: 1420-3049
• COBISS.SI-ID: 18462981

Licences

• License: CC BY 4.0, Creative Commons Attribution 4.0 International
• Link: http://creativecommons.org/licenses/by/4.0/
• Description: This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
• Licensing start date: 14.05.2016

Secondary language

• Language: Slovenian
• Keywords: Alzheimerjeva bolezen

Projects

• Funder: Other - Other funder or multiple funders
• Funding programme: Government of Spain
• Project number: SAF2016-65586-R

• Funder: Other - Other funder or multiple funders
• Funding programme: MH CZ- DRO
• Project number: UHHK 00179906