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Synthesis and biological evaluation of benzochromenopyrimidinones as cholinesterase inhibitors and potent antioxidant, non-hepatotoxic agents for Alzheimer's disease
ID
Dgachi, Youssef
(
Author
),
ID
Bautista-Aguilera, Oscar M.
(
Author
),
ID
Benchekroun, Mohamed
(
Author
),
ID
Martin, Hélène
(
Author
),
ID
Bonet, Alexandre
(
Author
),
ID
Knez, Damijan
(
Author
),
ID
Godyń, Justyna
(
Author
),
ID
Malawska, Barbara
(
Author
),
ID
Gobec, Stanislav
(
Author
),
ID
Chioua, Mourad
(
Author
),
ID
Janockova, Jana
(
Author
),
ID
Soukup, Ondrej
(
Author
),
ID
Chabchoub, Fakher
(
Author
),
ID
Marco-Contelles, José
(
Author
),
ID
Ismaili, Lhassane
(
Author
)
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MD5: F17E0E349251A9EC0CD5CFB4D3835FC6
URL - Source URL, Visit
http://www.mdpi.com/1420-3049/21/5/634
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Abstract
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
Views:
838
Downloads:
167
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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
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