Asproni, Battistina and Kehler, Jan and Simula, Sergio and Mura, Stefania and Porcu, Giovanna (2008) Synthesis and sar study of 2-substituted imidazo[2,1-b] [1,3]benzothiazoles and related compounds endowed with affinity for dopamine D2 receptors as potential antipsychotics. In: SardiniaChem 2008: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive, 30 Maggio 2008, Sassari, Italia. Conference or Workshop Item.
Typical antipsychotic agents such as chlorpromazine and haloperidol block the D2 subtype 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 D2 receptors 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.
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