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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

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.

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Abstract

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.

Item Type:Conference or Workshop Item (Poster)
ID Code:1054
Status:Published
Uncontrolled Keywords:Dopamine receptors, schizophrenia, antipsychotics
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Additional Information:Comitato Scientifico di SardiniaChem 2008: Giampaolo Giacomelli, Università di Sassari; Giovanna Delogu, CNR Sassari; Salvatore Cabiddu, Pier Paolo Piras, Università di Cagliari. Comitato Organizzatore: Andrea Porcheddu, Università di Sassari; Roberto Dallocchio, CNR Sassari; Stefania De Montis, Università di Cagliari. Realizzazione: Università di Sassari, Dipartimento di chimica e Facoltà di Scienze MFN; CNR, Istituto di chimica biomolecolare, sez. Sassari; Università di Cagliari; Agilent Technologies, Italia, s.p.a., Agenzia Sardegna; Sapio s.r.l.; Sigma-Aldrich s.r.l.; Carlo Erba Reagenti; Medinlab s.r.l.; VWR International s.r.l.
Deposited On:18 Aug 2009 10:04

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