TY  - JOUR
AU  - Andrić, Deana
AU  - Tovilović-Kovačević, Gordana
AU  - Roglić, Goran
AU  - Šoškić, Vukić
AU  - Tomić, Mirko
AU  - Kostić-Rajačić, Slađana V.
PY  - 2007
PY  - 2007
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/554
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-benzimidazole-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) D1 and D2 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 D2 and 5-HT1A receptors, with the most active of them having 34 and 170 time higher affinity than non-halogenated congeners in the D2 DA receptor radioassays (compounds 9.1b and 9.2b, respectively). Divergently, these compounds were without significant affinities for the D1 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. .
T2  - Journal of the Serbian Chemical Society
T1  - 6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje
T1  - 6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluation
IS  - 8-9
VL  - 72
DO  - 10.2298/JSC0709747A
SP  - 747
EP  - 755
UR  - https://hdl.handle.net/21.15107/rcub_ibiss_554
ER  - 

@article{
author = "Andrić, Deana and Tovilović-Kovačević, Gordana and Roglić, Goran and Šoškić, Vukić and Tomić, Mirko and Kostić-Rajačić, Slađana V.",
year = "2007, 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-benzimidazole-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) D1 and D2 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 D2 and 5-HT1A receptors, with the most active of them having 34 and 170 time higher affinity than non-halogenated congeners in the D2 DA receptor radioassays (compounds 9.1b and 9.2b, respectively). Divergently, these compounds were without significant affinities for the D1 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. .",
journal = "Journal of the Serbian Chemical Society",
title = "6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje, 6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluation",
number = "8-9",
volume = "72",
doi = "10.2298/JSC0709747A",
pages = "747-755",
url = "https://hdl.handle.net/21.15107/rcub_ibiss_554"
}

Andrić, D., Tovilović-Kovačević, G., Roglić, G., Šoškić, V., Tomić, M.,& Kostić-Rajačić, S. V.. (2007). 6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje. in Journal of the Serbian Chemical Society, 72(8-9), 747-755.
https://doi.org/10.2298/JSC0709747A
https://hdl.handle.net/21.15107/rcub_ibiss_554

Andrić D, Tovilović-Kovačević G, Roglić G, Šoškić V, Tomić M, Kostić-Rajačić SV. 6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje. in Journal of the Serbian Chemical Society. 2007;72(8-9):747-755.
doi:10.2298/JSC0709747A
https://hdl.handle.net/21.15107/rcub_ibiss_554 .

Andrić, Deana, Tovilović-Kovačević, Gordana, Roglić, Goran, Šoškić, Vukić, Tomić, Mirko, Kostić-Rajačić, Slađana V., "6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje" in Journal of the Serbian Chemical Society, 72, no. 8-9 (2007):747-755,
https://doi.org/10.2298/JSC0709747A .,
https://hdl.handle.net/21.15107/rcub_ibiss_554 .

TY  - JOUR
AU  - Andrić, Deana
AU  - Tovilović-Kovačević, Gordana
AU  - Roglić, Goran
AU  - Ignjatović, Đurđica
AU  - Šoškić, Vukić
AU  - Tomić, Mirko
AU  - Kostić-Rajačić, Slađana V.
PY  - 2007
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/553
AB  - Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, 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 (>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  - Belgrade: Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina
T1  - Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives
IS  - 5
VL  - 72
DO  - 10.2298/JSC0705429A
SP  - 429
EP  - 435
UR  - https://hdl.handle.net/21.15107/rcub_ibiss_553
ER  - 

@article{
author = "Andrić, Deana and Tovilović-Kovačević, Gordana and Roglić, Goran and Ignjatović, Đurđica and Šoškić, Vukić and Tomić, Mirko and Kostić-Rajačić, Slađana V.",
year = "2007",
abstract = "Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, 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 (>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 = "Belgrade: Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina, Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives",
number = "5",
volume = "72",
doi = "10.2298/JSC0705429A",
pages = "429-435",
url = "https://hdl.handle.net/21.15107/rcub_ibiss_553"
}

Andrić, D., Tovilović-Kovačević, G., Roglić, G., Ignjatović, Đ., Šoškić, V., Tomić, M.,& Kostić-Rajačić, S. V.. (2007). Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina. in Journal of the Serbian Chemical Society
Belgrade: Serbian Chemical Society., 72(5), 429-435.
https://doi.org/10.2298/JSC0705429A
https://hdl.handle.net/21.15107/rcub_ibiss_553

Andrić D, Tovilović-Kovačević G, Roglić G, Ignjatović Đ, Šoškić V, Tomić M, Kostić-Rajačić SV. Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina. in Journal of the Serbian Chemical Society. 2007;72(5):429-435.
doi:10.2298/JSC0705429A
https://hdl.handle.net/21.15107/rcub_ibiss_553 .

Andrić, Deana, Tovilović-Kovačević, Gordana, Roglić, Goran, Ignjatović, Đurđica, Šoškić, Vukić, Tomić, Mirko, Kostić-Rajačić, Slađana V., "Sinteza i farmakološko ispitivanje novih derivata N-(2-nitrofenil) piperazina" in Journal of the Serbian Chemical Society, 72, no. 5 (2007):429-435,
https://doi.org/10.2298/JSC0705429A .,
https://hdl.handle.net/21.15107/rcub_ibiss_553 .