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N-hydroxy-N-propargylamide derivatives of ferulic acid : inhibitors of cholinesterases and monoamine oxidases
ID
Bautista-Aguilera, Oscar M.
(
Avtor
),
ID
Alonso, José M.
(
Avtor
),
ID
Catto, Marco
(
Avtor
),
ID
Iriepa, Isabel
(
Avtor
),
ID
Knez, Damijan
(
Avtor
),
ID
Gobec, Stanislav
(
Avtor
),
ID
Marco-Contelles, José
(
Avtor
)
PDF - Predstavitvena datoteka,
prenos
(792,16 KB)
MD5: 43DB8F68B71C521F26574F9486E9F3A9
URL - Izvorni URL, za dostop obiščite
https://www.mdpi.com/1420-3049/27/21/7437
Galerija slik
Izvleček
Alzheimer’s disease (AD) is a complex disorder characterized by impaired neurotransmission in cholinergic and monoaminergic neurons, which, in combination with the accumulation of misfolded proteins and increased oxidative stress, leads to the typical features of the disease at the biomolecular level. Given the limited therapeutic success of approved drugs, it is imperative to explore rationally supported therapeutic approaches to combat this disease. The search for novel scaffolds that bind to different receptors and inhibit AD disease-related enzymes could lead to new therapeutic solutions. Here, we describe N-hydroxy-N-propargylamide hybrids 1–6, which were designed by combining the structures of Contilisant—a multifunctional anti-AD ligand—and ferulic acid, a natural antioxidant with various other biological activities. Among the synthesized compounds, we identified compound 4 as a micromolar inhibitor of hAChE with a potent radical-scavenging capacity comparable to resveratrol and Trolox. In addition, compound 4 chelated copper(II) ions associated with amyloid β pathology, mitochondrial dysfunction, and oxidative stress. The promising in vitro activity combined with favorable drug-like properties and predicted blood‒brain barrier permeability make compound 4 a multifunctional ligand that merits further studies at the biochemical and cellular levels.
Jezik:
Angleški jezik
Ključne besede:
cholinesterases
,
ferulic acid
,
molecular modelling
,
monoamine oxidase
,
radical-scavenger
,
antioxidant
Vrsta gradiva:
Članek v reviji
Tipologija:
1.01 - Izvirni znanstveni članek
Organizacija:
FFA - Fakulteta za farmacijo
Status publikacije:
Objavljeno
Različica publikacije:
Objavljena publikacija
Leto izida:
2022
Št. strani:
18 str.
Številčenje:
Vol. 27, iss. 21, art. 7437
PID:
20.500.12556/RUL-142354
UDK:
616.894
ISSN pri članku:
1420-3049
DOI:
10.3390/molecules27217437
COBISS.SI-ID:
127684867
Datum objave v RUL:
02.11.2022
Število ogledov:
474
Število prenosov:
71
Metapodatki:
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Objavi na:
Gradivo je del revije
Naslov:
Molecules
Skrajšan naslov:
Molecules
Založnik:
MDPI
ISSN:
1420-3049
COBISS.SI-ID:
18462981
Licence
Licenca:
CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
Povezava:
http://creativecommons.org/licenses/by/4.0/deed.sl
Opis:
To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.
Sekundarni jezik
Jezik:
Slovenski jezik
Ključne besede:
holinesteraze
,
ferulna kislina
,
molekularno modeliranje
,
monoaminooksidaza
,
lovilec radikalov
,
antioksidant
Projekti
Financer:
ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
Številka projekta:
P1-0208-2015
Naslov:
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin
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