TY  - JOUR
AU  - Tomić, Mirko
AU  - Vasković, Djurdjica
AU  - Tovilović, Gordana
AU  - Andrić, Deana
AU  - Penjišević, Jelena
AU  - Kostić Rajačić, Slađana
PY  - 2011
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/916
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 = "Tomić, Mirko and Vasković, 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"
}

Tomić, M., Vasković, 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

Tomić M, Vasković 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 .

Tomić, Mirko, Vasković, 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 . .

TY  - JOUR
AU  - Andrić, Deana
AU  - Tovilović, Gordana
AU  - Roglić, Goran
AU  - Vasković, Đurđica
AU  - Šoškić, Vukić
AU  - Tomić, Mirko
AU  - Kostić Rajačić, Slađana
PY  - 2007
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/313
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  - Serbian Chemical Society
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 Tomić, Mirko and Kostić Rajačić, Slađana",
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 = "Serbian Chemical Society",
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., Tomić, 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 Society., 72(5), 429-435.
https://doi.org/10.2298/JSC0705429A

Andrić D, Tovilović G, Roglić G, Vasković Đ, Šoškić V, Tomić 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, Tomić, 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 . .