TY  - CONF
AU  - Bondžić, Aleksandra
AU  - Jovanović, Dunja
AU  - Džambaski, Zdravko
AU  - Filipović, Ana
AU  - Bondžić, Bojan
PY  - 2022
UR  - https://vinar.vin.bg.ac.rs/handle/123456789/12366
AB  - The goal of this work was to investigate the inhibitory potency of three derivates of 2- phenyl-1,2,3,4-tetrahydroisoquinoline (THIQ) with different substituents at C3 and C4 positions, namely 65P,71P and 66P, toward two cholinergic enzymes, acetyl and butyrylcholinesterase. The screening test showed that only compound 65P possesses inhibition activity higher than 50 % at 10 μM concentration toward both enzymes. The inhibition potency obtained at 10 μM of THIQ was correlated with differences in THIQ’s structures in order to predict the structure-activity relationship. It was found that the introduction of the methoxy group at positions C3 and C4 led to decreased inhibition potency, while the removing of fluorine atom from the benzene ring increases selectivity toward acetylcholinesterase. The IC50 value gained during the evaluation of inhibition activity of 65P indicated strong inhibition potency of this compound, while Hill’s coefficient ~ 1 indicated the non-existence of cooperativity and one binding site on both enzymes clearly indicating that THIQ could be promising therapeutic drugs in the treatment of Alzheimer’s disease.
PB  - Belgrade : Society of Physical Chemists of Serbia
C3  - PHYSICAL CHEMISTRY 2022 : 16th International Conference on Fundamental and Applied Aspects of Physical Chemistry : Book of abstracts
T1  - New derivates of 2-phenyl-1,2,3,4-tetrahydroizoquinoline as dual inhibitors of cholinergic enzymes
SP  - 170
EP  - 170
UR  - https://hdl.handle.net/21.15107/rcub_vinar_12366
ER  - 

@conference{
author = "Bondžić, Aleksandra and Jovanović, Dunja and Džambaski, Zdravko and Filipović, Ana and Bondžić, Bojan",
year = "2022",
abstract = "The goal of this work was to investigate the inhibitory potency of three derivates of 2- phenyl-1,2,3,4-tetrahydroisoquinoline (THIQ) with different substituents at C3 and C4 positions, namely 65P,71P and 66P, toward two cholinergic enzymes, acetyl and butyrylcholinesterase. The screening test showed that only compound 65P possesses inhibition activity higher than 50 % at 10 μM concentration toward both enzymes. The inhibition potency obtained at 10 μM of THIQ was correlated with differences in THIQ’s structures in order to predict the structure-activity relationship. It was found that the introduction of the methoxy group at positions C3 and C4 led to decreased inhibition potency, while the removing of fluorine atom from the benzene ring increases selectivity toward acetylcholinesterase. The IC50 value gained during the evaluation of inhibition activity of 65P indicated strong inhibition potency of this compound, while Hill’s coefficient ~ 1 indicated the non-existence of cooperativity and one binding site on both enzymes clearly indicating that THIQ could be promising therapeutic drugs in the treatment of Alzheimer’s disease.",
publisher = "Belgrade : Society of Physical Chemists of Serbia",
journal = "PHYSICAL CHEMISTRY 2022 : 16th International Conference on Fundamental and Applied Aspects of Physical Chemistry : Book of abstracts",
title = "New derivates of 2-phenyl-1,2,3,4-tetrahydroizoquinoline as dual inhibitors of cholinergic enzymes",
pages = "170-170",
url = "https://hdl.handle.net/21.15107/rcub_vinar_12366"
}

Bondžić, A., Jovanović, D., Džambaski, Z., Filipović, A.,& Bondžić, B.. (2022). New derivates of 2-phenyl-1,2,3,4-tetrahydroizoquinoline as dual inhibitors of cholinergic enzymes. in PHYSICAL CHEMISTRY 2022 : 16th International Conference on Fundamental and Applied Aspects of Physical Chemistry : Book of abstracts
Belgrade : Society of Physical Chemists of Serbia., 170-170.
https://hdl.handle.net/21.15107/rcub_vinar_12366

Bondžić A, Jovanović D, Džambaski Z, Filipović A, Bondžić B. New derivates of 2-phenyl-1,2,3,4-tetrahydroizoquinoline as dual inhibitors of cholinergic enzymes. in PHYSICAL CHEMISTRY 2022 : 16th International Conference on Fundamental and Applied Aspects of Physical Chemistry : Book of abstracts. 2022;:170-170.
https://hdl.handle.net/21.15107/rcub_vinar_12366 .

Bondžić, Aleksandra, Jovanović, Dunja, Džambaski, Zdravko, Filipović, Ana, Bondžić, Bojan, "New derivates of 2-phenyl-1,2,3,4-tetrahydroizoquinoline as dual inhibitors of cholinergic enzymes" in PHYSICAL CHEMISTRY 2022 : 16th International Conference on Fundamental and Applied Aspects of Physical Chemistry : Book of abstracts (2022):170-170,
https://hdl.handle.net/21.15107/rcub_vinar_12366 .