Typical antipsychotic agents such as chlorpromazine and haloperidol block the D2subtype of dopamine receptors in a direct relation to their clinical potency. In this context we have developed a series of (1,2-diphenyl-imidazolyl)piperazine derivatives (1) that are endowed with substantial affinities for both dopamine D2receptors as well as 5-HT1A and 5-HT2A serotonin receptors, compound 1a (R = o-OCH3) of which is representative. We have extended our study on other series of compounds derived from 1 both modifying the 1,2-diphenyl motif attached to the imidazole core, and the phenyl-piperazine moiety.
Synthesis and sar study of 2-substituted imidazo[2,1-b] [1,3]benzothiazoles and related compounds endowed with affinity for dopamine D2receptors as potential antipsychotics / Asproni, Battistina; Kehler, Jan; Mura, Stefania; Porcu, Giovanna; Simula, Sergio. - (2008). (Intervento presentato al convegno SardiniaChem 2008: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive).
Synthesis and sar study of 2-substituted imidazo[2,1-b] [1,3]benzothiazoles and related compounds endowed with affinity for dopamine D2receptors as potential antipsychotics
Asproni, Battistina;Mura, Stefania;Porcu, Giovanna;
2008-01-01
Abstract
Typical antipsychotic agents such as chlorpromazine and haloperidol block the D2subtype of dopamine receptors in a direct relation to their clinical potency. In this context we have developed a series of (1,2-diphenyl-imidazolyl)piperazine derivatives (1) that are endowed with substantial affinities for both dopamine D2receptors as well as 5-HT1A and 5-HT2A serotonin receptors, compound 1a (R = o-OCH3) of which is representative. We have extended our study on other series of compounds derived from 1 both modifying the 1,2-diphenyl motif attached to the imidazole core, and the phenyl-piperazine moiety.File | Dimensione | Formato | |
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