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6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanje

dc.creatorAndrić, Deana
dc.creatorTovilović, Gordana
dc.creatorRoglić, Goran
dc.creatorŠoškić, Vukić
dc.creatorTomić, Mirko
dc.creatorKostić Rajačić, Slađana
dc.date.accessioned2019-01-30T17:15:45Z
dc.date.available2019-01-30T17:15:45Z
dc.date.issued2007
dc.identifier.issn0352-5139
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/323
dc.description.abstractEight 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. .en
dc.description.abstractSintetisano 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. .sr
dc.publisherSerbian Chemical Society
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/143032/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/142009/RS//
dc.rightsopenAccess
dc.sourceJournal of the Serbian Chemical Society
dc.subjectarylpiperazinesen
dc.subjectbenzimidazole-2-thionesen
dc.subjectdopamine receptorsen
dc.subjectserotonin receptorsen
dc.title6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluationen
dc.title6-[2-(4-arilpiperazin-1-il)etil]-4-halo-1,3-dihidro-2h-benzimidazol-2-tioni - sinteza i farmakološko ispitivanjesr
dc.typearticle
dc.rights.licenseBY-NC-ND
dcterms.abstractКостић Рајачић, Слађана; Роглић, Горан; Товиловић, Гордана; Томић, Мирко; Шошкић, Вукић; Aндрић, Деана; 6-[2-(4-арилпиперазин-1-ил)етил]-4-хало-1,3-дихидро-2х-бензимидазол-2-тиони - синтеза и фармаколошко испитивање; 6-[2-(4-арилпиперазин-1-ил)етил]-4-хало-1,3-дихидро-2х-бензимидазол-2-тиони - синтеза и фармаколошко испитивање;
dc.citation.volume72
dc.citation.issue8-9
dc.citation.spage747
dc.citation.epage755
dc.citation.other72(8-9): 747-755
dc.citation.rankM23
dc.identifier.doi10.2298/JSC0709747A
dc.identifier.rcubConv_234
dc.identifier.fulltexthttp://cer.ihtm.bg.ac.rs//bitstream/id/9001/321.pdf
dc.identifier.scopus2-s2.0-34548435274
dc.type.versionpublishedVersion


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