Tomic, Mirko

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  • Tomic, Mirko (5)
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Author's Bibliography

The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside

Ignjatović, Đurđica; Milutinovic, Danijela Vojnovic; Nikolić-Kokić, Aleksandra; Slavic, Marija; Andrić, Deana; Tomic, Mirko; Kostić-Rajačić, Slađana

(Elsevier Science Bv, Amsterdam, 2012)

TY  - JOUR
AU  - Ignjatović, Đurđica
AU  - Milutinovic, Danijela Vojnovic
AU  - Nikolić-Kokić, Aleksandra
AU  - Slavic, Marija
AU  - Andrić, Deana
AU  - Tomic, Mirko
AU  - Kostić-Rajačić, Slađana
PY  - 2012
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/1289
AB  - A group of sixteen arylpiperazines had been previously synthesized and evaluated for atypical antipsychotic activity. Here we examined these compounds for their neuroprotective capacity. The affinity and agonist/antagonist action of the arylpiperazines at dopamine hD(2S) receptors were determined in vitro on membranes from stably transfected CHO-hD(2S) cell line. The assays for cell viability and antioxidative capacity (total glutathione and total superoxide dismutase activity), amount of nitric oxide and superoxide radicals, as well as influence on prosurvival pathways (Akt and ERK), were performed on the human neuroblastoma cell line SH-SY5Y. Cell death was induced by oxidative or nitrosative stress, or by growing cells in the medium deprived of serum. Only four of the arylpiperazines exhibited notable neuroprotection against cell death induced by sodium nitroprusside. Two of these arylpiperazines induced elevations of pAkt, while two other compounds reduced the levels of pErk, whereas these actions are considered to support the cell survival. The benzimidazole heteroaryl-group, that mimics catechol moiety of the dopamine molecule, might be the prerequisite structure for the neuroprotective action of these ligands. It is postulated that neuroprotection was acquired also by elevation of endogenous glutathione or total superoxide dismutase activity. (C) 2012 Elsevier B.V. All rights reserved.
PB  - Elsevier Science Bv, Amsterdam
T2  - European Journal of Pharmacology
T1  - The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside
VL  - 683
IS  - 1-3
SP  - 93
EP  - 100
DO  - 10.1016/j.ejphar.2012.03.011
ER  - 
@article{
author = "Ignjatović, Đurđica and Milutinovic, Danijela Vojnovic and Nikolić-Kokić, Aleksandra and Slavic, Marija and Andrić, Deana and Tomic, Mirko and Kostić-Rajačić, Slađana",
year = "2012",
abstract = "A group of sixteen arylpiperazines had been previously synthesized and evaluated for atypical antipsychotic activity. Here we examined these compounds for their neuroprotective capacity. The affinity and agonist/antagonist action of the arylpiperazines at dopamine hD(2S) receptors were determined in vitro on membranes from stably transfected CHO-hD(2S) cell line. The assays for cell viability and antioxidative capacity (total glutathione and total superoxide dismutase activity), amount of nitric oxide and superoxide radicals, as well as influence on prosurvival pathways (Akt and ERK), were performed on the human neuroblastoma cell line SH-SY5Y. Cell death was induced by oxidative or nitrosative stress, or by growing cells in the medium deprived of serum. Only four of the arylpiperazines exhibited notable neuroprotection against cell death induced by sodium nitroprusside. Two of these arylpiperazines induced elevations of pAkt, while two other compounds reduced the levels of pErk, whereas these actions are considered to support the cell survival. The benzimidazole heteroaryl-group, that mimics catechol moiety of the dopamine molecule, might be the prerequisite structure for the neuroprotective action of these ligands. It is postulated that neuroprotection was acquired also by elevation of endogenous glutathione or total superoxide dismutase activity. (C) 2012 Elsevier B.V. All rights reserved.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "European Journal of Pharmacology",
title = "The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside",
volume = "683",
number = "1-3",
pages = "93-100",
doi = "10.1016/j.ejphar.2012.03.011"
}
Ignjatović, Đ., Milutinovic, D. V., Nikolić-Kokić, A., Slavic, M., Andrić, D., Tomic, M.,& Kostić-Rajačić, S.. (2012). The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside. in European Journal of Pharmacology
Elsevier Science Bv, Amsterdam., 683(1-3), 93-100.
https://doi.org/10.1016/j.ejphar.2012.03.011
Ignjatović Đ, Milutinovic DV, Nikolić-Kokić A, Slavic M, Andrić D, Tomic M, Kostić-Rajačić S. The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside. in European Journal of Pharmacology. 2012;683(1-3):93-100.
doi:10.1016/j.ejphar.2012.03.011 .
Ignjatović, Đurđica, Milutinovic, Danijela Vojnovic, Nikolić-Kokić, Aleksandra, Slavic, Marija, Andrić, Deana, Tomic, Mirko, Kostić-Rajačić, Slađana, "The mechanisms responsible for neuroprotective capacity of arylpiperazine dopaminergic ligands against cell death induced by sodium nitroprusside" in European Journal of Pharmacology, 683, no. 1-3 (2012):93-100,
https://doi.org/10.1016/j.ejphar.2012.03.011 . .
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Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands

Tomic, Mirko; Vaskovic, Djurdjica; Tovilović, Gordana; Andrić, Deana; Penjišević, Jelena; Kostić-Rajačić, Slađana

(Wiley-Blackwell, Malden, 2011)

TY  - JOUR
AU  - Tomic, Mirko
AU  - Vaskovic, Djurdjica
AU  - Tovilović, Gordana
AU  - Andrić, Deana
AU  - Penjišević, Jelena
AU  - Kostić-Rajačić, Slađana
PY  - 2011
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/1337
AB  - Five groups of previously synthesized and initially screened non-substituted and 4-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles were estimated for their in-vitro binding affinities at the rat D-2, 5-HT2A, and alpha(1)-adrenergic receptors. Among all these compounds, 2-methoxyphenyl and 2-chlorophenyl piperazines demonstrate the highest affinities for the tested receptors. The effects of 4-halogenation of benzimidazoles reveal that substitution with brominemay greatly increase the affinity of the compounds for the studied receptors, while the effect of substitution with chlorine is less remarkable. Most of the tested components show 5-HT2A/D-2 pK(i) binding ratios slightly above or less than 1, while only 4-chloro-6-(2-{4-[3-(trifluoromethyl) phenyl]piperazin-1-yl}ethyl)-1H-benzimidazole expresses an appropriate higher binding ratio (1.14), which was indicated for atypical neuroleptics. This compound exhibits a non-cataleptic action in rats and prevents d-amphetamine-induced hyperlocomotion in mice, which suggest its atypical antipsychotic potency.
PB  - Wiley-Blackwell, Malden
T2  - Archiv der Pharmazie
T1  - Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands
VL  - 344
IS  - 5
SP  - 287
EP  - 291
DO  - 10.1002/ardp.200900168
ER  - 
@article{
author = "Tomic, Mirko and Vaskovic, Djurdjica and Tovilović, Gordana and Andrić, Deana and Penjišević, Jelena and Kostić-Rajačić, Slađana",
year = "2011",
abstract = "Five groups of previously synthesized and initially screened non-substituted and 4-halogenated arylpiperazin-1-yl-ethyl-benzimidazoles were estimated for their in-vitro binding affinities at the rat D-2, 5-HT2A, and alpha(1)-adrenergic receptors. Among all these compounds, 2-methoxyphenyl and 2-chlorophenyl piperazines demonstrate the highest affinities for the tested receptors. The effects of 4-halogenation of benzimidazoles reveal that substitution with brominemay greatly increase the affinity of the compounds for the studied receptors, while the effect of substitution with chlorine is less remarkable. Most of the tested components show 5-HT2A/D-2 pK(i) binding ratios slightly above or less than 1, while only 4-chloro-6-(2-{4-[3-(trifluoromethyl) phenyl]piperazin-1-yl}ethyl)-1H-benzimidazole expresses an appropriate higher binding ratio (1.14), which was indicated for atypical neuroleptics. This compound exhibits a non-cataleptic action in rats and prevents d-amphetamine-induced hyperlocomotion in mice, which suggest its atypical antipsychotic potency.",
publisher = "Wiley-Blackwell, Malden",
journal = "Archiv der Pharmazie",
title = "Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands",
volume = "344",
number = "5",
pages = "287-291",
doi = "10.1002/ardp.200900168"
}
Tomic, M., Vaskovic, D., Tovilović, G., Andrić, D., Penjišević, J.,& Kostić-Rajačić, S.. (2011). Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands. in Archiv der Pharmazie
Wiley-Blackwell, Malden., 344(5), 287-291.
https://doi.org/10.1002/ardp.200900168
Tomic M, Vaskovic D, Tovilović G, Andrić D, Penjišević J, Kostić-Rajačić S. Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands. in Archiv der Pharmazie. 2011;344(5):287-291.
doi:10.1002/ardp.200900168 .
Tomic, Mirko, Vaskovic, Djurdjica, Tovilović, Gordana, Andrić, Deana, Penjišević, Jelena, Kostić-Rajačić, Slađana, "Pharmacological Evaluation of Halogenated and Non-halogenated Arylpiperazin-1-yl-ethyl-benzimidazoles as D-2 and 5-HT2A Receptor Ligands" in Archiv der Pharmazie, 344, no. 5 (2011):287-291,
https://doi.org/10.1002/ardp.200900168 . .
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Two new phenylpiperazines with atypical antipsychotic potential

Tomic, Mirko; Ignjatović, Đurđica; Tovijovic, Gordana; Andrić, Deana; Roglić, Goran; Kostić-Rajačić, Slađana

(Pergamon-Elsevier Science Ltd, Oxford, 2007)

TY  - JOUR
AU  - Tomic, Mirko
AU  - Ignjatović, Đurđica
AU  - Tovijovic, Gordana
AU  - Andrić, Deana
AU  - Roglić, Goran
AU  - Kostić-Rajačić, Slađana
PY  - 2007
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/886
AB  - Two new series of substituted arylpiperazines with heterocyclic 3-propoxy-benzimidazole or 3-propoxy-benzimidazole-2-thione groups were synthesized and their in vitro binding affinities for the D,, 5-HT1A, 5-HT2A, and alpha-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT2A/D-2 pK(i) binding ratios proposed for atypical neuroleptics. As to their behavioral screening on rodents, both compounds exhibited a non-cataleptic action in rats and antagonized D-amphetamine-induced hyperlocomotion in mice, suggesting their possible atypical antipsychotic potency. (c) 2007 Elsevier Ltd. All rights reserved.
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Bioorganic and Medicinal Chemistry Letters
T1  - Two new phenylpiperazines with atypical antipsychotic potential
VL  - 17
IS  - 21
SP  - 5749
EP  - 5753
DO  - 10.1016/j.bmcl.2007.08.066
ER  - 
@article{
author = "Tomic, Mirko and Ignjatović, Đurđica and Tovijovic, Gordana and Andrić, Deana and Roglić, Goran and Kostić-Rajačić, Slađana",
year = "2007",
abstract = "Two new series of substituted arylpiperazines with heterocyclic 3-propoxy-benzimidazole or 3-propoxy-benzimidazole-2-thione groups were synthesized and their in vitro binding affinities for the D,, 5-HT1A, 5-HT2A, and alpha-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT2A/D-2 pK(i) binding ratios proposed for atypical neuroleptics. As to their behavioral screening on rodents, both compounds exhibited a non-cataleptic action in rats and antagonized D-amphetamine-induced hyperlocomotion in mice, suggesting their possible atypical antipsychotic potency. (c) 2007 Elsevier Ltd. All rights reserved.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Bioorganic and Medicinal Chemistry Letters",
title = "Two new phenylpiperazines with atypical antipsychotic potential",
volume = "17",
number = "21",
pages = "5749-5753",
doi = "10.1016/j.bmcl.2007.08.066"
}
Tomic, M., Ignjatović, Đ., Tovijovic, G., Andrić, D., Roglić, G.,& Kostić-Rajačić, S.. (2007). Two new phenylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters
Pergamon-Elsevier Science Ltd, Oxford., 17(21), 5749-5753.
https://doi.org/10.1016/j.bmcl.2007.08.066
Tomic M, Ignjatović Đ, Tovijovic G, Andrić D, Roglić G, Kostić-Rajačić S. Two new phenylpiperazines with atypical antipsychotic potential. in Bioorganic and Medicinal Chemistry Letters. 2007;17(21):5749-5753.
doi:10.1016/j.bmcl.2007.08.066 .
Tomic, Mirko, Ignjatović, Đurđica, Tovijovic, Gordana, Andrić, Deana, Roglić, Goran, Kostić-Rajačić, Slađana, "Two new phenylpiperazines with atypical antipsychotic potential" in Bioorganic and Medicinal Chemistry Letters, 17, no. 21 (2007):5749-5753,
https://doi.org/10.1016/j.bmcl.2007.08.066 . .
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6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation

Andrić, Deana; Tovilović, Gordana; Roglić, Goran; Šoškić, Vukić; Tomic, Mirko; Kostić-Rajačić, Slađana

(Serbian Chemical Soc, Belgrade, 2007)

TY  - JOUR
AU  - Andrić, Deana
AU  - Tovilović, Gordana
AU  - Roglić, Goran
AU  - Šoškić, Vukić
AU  - Tomic, Mirko
AU  - Kostić-Rajačić, Slađana
PY  - 2007
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/877
AB  - Eight new compounds with halogen atom introduced into the benzimidazole-2-thione dopaminergic pharmacophore of 5-[2-(4-arylpiperazin-1-yl)ethyl]-1,3-dihydro-2H-benzi -2-thiones with the arylpiperazine part of the molecule being selected according to known structure-affinity requirements, have been synthesized. All the new compounds were evaluated for the in vitro binding affinity at the dopamine (DA) D-1 and D-2 and serotonin 5-HT1A receptors by the competitive radioassays, performed on synaptosomal membranes prepared from fresh bovine caudate nuclei and hippocampi. All the new compounds were strong competitors for the binding of the radioligands to the D-2 and 5-HT1A receptors, with the most active of them having 34 and 170 time higher affinity than non-halogenated congeners in the D-2 DA receptor radioassays (compounds 9.1b and 9.2b, respectively). Divergently, these compounds were without significant affinities for the D-1 DA receptors.
AB  - Sintetisano je osam novih jedinjenja kod kojih je atom halogena uveden u benzimidazol-2-tionsku dopaminergičku farmakoforu 5-[2-(4-arilpiperazin-1-il)etil]-1,3-dihidro-2N-benzimidazol-2-tiona sa arilpiperazinskim delom molekula izabranim shodno pozna- tim zahtevima o odnosu strukture i reaktivnosti. Za sva novosintetisana jedinjenja je određen afinitet vezivanja za dopaminske (D1 i D2) i 5-NT1A receptore u in vitro eksperimentima kompeticije sa radioligandima. Kao izvor dopaminskih i 5-NT1A receptora su korištene sinaptozomalne membrane izolovane iz goveđeg nukleusa kaudatusa i hipokampusa. Sva novosintetisana jedinjenja pokazala su se kao jaki kompetitori [3H]spiperona i [3H]8-OH-DPAT, od kojih najaktivnija (9.1b i 9.2b) poseduju 34 i 170 puta veći afinitet ka D2 DA receptorima od polaznih, nehalogenovanih jedinjenja. Sa druge strane, ova jedinjenja ne poseduju značajan afinitet ka D1 dopaminskim receptorima. .
PB  - Serbian Chemical Soc, Belgrade
T2  - Journal of the Serbian Chemical Society
T1  - 6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation
T1  - 6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje
VL  - 72
IS  - 8-9
SP  - 747
EP  - 755
DO  - 10.2298/JSC0709747A
ER  - 
@article{
author = "Andrić, Deana and Tovilović, Gordana and Roglić, Goran and Šoškić, Vukić and Tomic, Mirko and Kostić-Rajačić, Slađana",
year = "2007",
abstract = "Eight new compounds with halogen atom introduced into the benzimidazole-2-thione dopaminergic pharmacophore of 5-[2-(4-arylpiperazin-1-yl)ethyl]-1,3-dihydro-2H-benzi -2-thiones with the arylpiperazine part of the molecule being selected according to known structure-affinity requirements, have been synthesized. All the new compounds were evaluated for the in vitro binding affinity at the dopamine (DA) D-1 and D-2 and serotonin 5-HT1A receptors by the competitive radioassays, performed on synaptosomal membranes prepared from fresh bovine caudate nuclei and hippocampi. All the new compounds were strong competitors for the binding of the radioligands to the D-2 and 5-HT1A receptors, with the most active of them having 34 and 170 time higher affinity than non-halogenated congeners in the D-2 DA receptor radioassays (compounds 9.1b and 9.2b, respectively). Divergently, these compounds were without significant affinities for the D-1 DA receptors., Sintetisano je osam novih jedinjenja kod kojih je atom halogena uveden u benzimidazol-2-tionsku dopaminergičku farmakoforu 5-[2-(4-arilpiperazin-1-il)etil]-1,3-dihidro-2N-benzimidazol-2-tiona sa arilpiperazinskim delom molekula izabranim shodno pozna- tim zahtevima o odnosu strukture i reaktivnosti. Za sva novosintetisana jedinjenja je određen afinitet vezivanja za dopaminske (D1 i D2) i 5-NT1A receptore u in vitro eksperimentima kompeticije sa radioligandima. Kao izvor dopaminskih i 5-NT1A receptora su korištene sinaptozomalne membrane izolovane iz goveđeg nukleusa kaudatusa i hipokampusa. Sva novosintetisana jedinjenja pokazala su se kao jaki kompetitori [3H]spiperona i [3H]8-OH-DPAT, od kojih najaktivnija (9.1b i 9.2b) poseduju 34 i 170 puta veći afinitet ka D2 DA receptorima od polaznih, nehalogenovanih jedinjenja. Sa druge strane, ova jedinjenja ne poseduju značajan afinitet ka D1 dopaminskim receptorima. .",
publisher = "Serbian Chemical Soc, Belgrade",
journal = "Journal of the Serbian Chemical Society",
title = "6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation, 6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje",
volume = "72",
number = "8-9",
pages = "747-755",
doi = "10.2298/JSC0709747A"
}
Andrić, D., Tovilović, G., Roglić, G., Šoškić, V., Tomic, M.,& Kostić-Rajačić, S.. (2007). 6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation. in Journal of the Serbian Chemical Society
Serbian Chemical Soc, Belgrade., 72(8-9), 747-755.
https://doi.org/10.2298/JSC0709747A
Andrić D, Tovilović G, Roglić G, Šoškić V, Tomic M, Kostić-Rajačić S. 6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation. in Journal of the Serbian Chemical Society. 2007;72(8-9):747-755.
doi:10.2298/JSC0709747A .
Andrić, Deana, Tovilović, Gordana, Roglić, Goran, Šoškić, Vukić, Tomic, Mirko, Kostić-Rajačić, Slađana, "6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation" in Journal of the Serbian Chemical Society, 72, no. 8-9 (2007):747-755,
https://doi.org/10.2298/JSC0709747A . .
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Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives

Andrić, Deana; Tovilović, Gordana; Roglić, Goran; Vasković, Đurđica; Šoškić, Vukić; Tomic, Mirko; Kostić-Rajačić, Slađana

(Serbian Chemical Soc, Belgrade, 2007)

TY  - JOUR
AU  - Andrić, Deana
AU  - Tovilović, Gordana
AU  - Roglić, Goran
AU  - Vasković, Đurđica
AU  - Šoškić, Vukić
AU  - Tomic, Mirko
AU  - Kostić-Rajačić, Slađana
PY  - 2007
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/845
AB  - Six newly synthesized heterocyclic (2-nitroplienyl)piperazines. with a specific structure of the heteroaryl group, which mimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and alpha I receptors. All compounds with a benzimidazole group had a 5-HT2A/D-2 receptors binding ratio characteristic for atypical neuroleptics ( gt  1, pK(i) values). Compound 7e, 4-bromo-6-{2-[4-(2-nitrophenyl)piperazin-1-yl]etliyl}-1H-benziniidazole, expressed higher affinities for all receptor classes than clozapine. Also, it exhibited the best characteristic for atypical neuroleptics and presents a compound with the best profile for further in vivo investigations.
AB  - Sintetisano je šest heterocikličnih (2-nitrofenil)piperazina sa specifičnom heteroaril grupom, koja podražava kateholsku grupu dopamina (benzimidazoli i supstituisani benzimidazoli), i ispitan je njihov afinitet ka dopaminskim, serotoninskim i _1 receptorima. Sva jedinjenja sa benzimidazolskim grupama su pokazala 5-HT 1A/D2 odnos vezivanja karakterističan za atipične neuroleptike ( gt 1, pK i vrednosti). Jedinjenje 7c, 4-bromo-6-{2-_4-(2-nitrofenil)piperazin-1-il_etil}-1H-benzimidazol, pokazalo je izraženiji afinitet ka svim klasama receptora u poređenju sa klozapinom i takođe predstavlja jedinjenje sa najboljim karakteristikama za dalja in vivo istraživanja.
PB  - Serbian Chemical Soc, Belgrade
T2  - Journal of the Serbian Chemical Society
T1  - Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives
T1  - Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina
VL  - 72
IS  - 5
SP  - 429
EP  - 435
DO  - 10.2298/JSC0705429A
ER  - 
@article{
author = "Andrić, Deana and Tovilović, Gordana and Roglić, Goran and Vasković, Đurđica and Šoškić, Vukić and Tomic, Mirko and Kostić-Rajačić, Slađana",
year = "2007",
abstract = "Six newly synthesized heterocyclic (2-nitroplienyl)piperazines. with a specific structure of the heteroaryl group, which mimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and alpha I receptors. All compounds with a benzimidazole group had a 5-HT2A/D-2 receptors binding ratio characteristic for atypical neuroleptics ( gt  1, pK(i) values). Compound 7e, 4-bromo-6-{2-[4-(2-nitrophenyl)piperazin-1-yl]etliyl}-1H-benziniidazole, expressed higher affinities for all receptor classes than clozapine. Also, it exhibited the best characteristic for atypical neuroleptics and presents a compound with the best profile for further in vivo investigations., Sintetisano je šest heterocikličnih (2-nitrofenil)piperazina sa specifičnom heteroaril grupom, koja podražava kateholsku grupu dopamina (benzimidazoli i supstituisani benzimidazoli), i ispitan je njihov afinitet ka dopaminskim, serotoninskim i _1 receptorima. Sva jedinjenja sa benzimidazolskim grupama su pokazala 5-HT 1A/D2 odnos vezivanja karakterističan za atipične neuroleptike ( gt 1, pK i vrednosti). Jedinjenje 7c, 4-bromo-6-{2-_4-(2-nitrofenil)piperazin-1-il_etil}-1H-benzimidazol, pokazalo je izraženiji afinitet ka svim klasama receptora u poređenju sa klozapinom i takođe predstavlja jedinjenje sa najboljim karakteristikama za dalja in vivo istraživanja.",
publisher = "Serbian Chemical Soc, Belgrade",
journal = "Journal of the Serbian Chemical Society",
title = "Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives, Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina",
volume = "72",
number = "5",
pages = "429-435",
doi = "10.2298/JSC0705429A"
}
Andrić, D., Tovilović, G., Roglić, G., Vasković, Đ., Šoškić, V., Tomic, M.,& Kostić-Rajačić, S.. (2007). Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives. in Journal of the Serbian Chemical Society
Serbian Chemical Soc, Belgrade., 72(5), 429-435.
https://doi.org/10.2298/JSC0705429A
Andrić D, Tovilović G, Roglić G, Vasković Đ, Šoškić V, Tomic M, Kostić-Rajačić S. Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives. in Journal of the Serbian Chemical Society. 2007;72(5):429-435.
doi:10.2298/JSC0705429A .
Andrić, Deana, Tovilović, Gordana, Roglić, Goran, Vasković, Đurđica, Šoškić, Vukić, Tomic, Mirko, Kostić-Rajačić, Slađana, "Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives" in Journal of the Serbian Chemical Society, 72, no. 5 (2007):429-435,
https://doi.org/10.2298/JSC0705429A . .
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