Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile

Novel arylsulfonamides were identified as high-affinity dopamine D3 and D2 receptor ligands. Some derivatives were found to be active in antipsychotic tests in vivo. A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several membe...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 17; no. 19; pp. 5340 - 5344
Main Authors:	Ágai-Csongor, Éva, Nógrádi, Katalin, Galambos, János, Vágó, István, Bielik, Attila, Magdó, Ildikó, Ignácz-Szendrei, Györgyi, Keserű, György Miklós, Greiner, István, Laszlovszky, István, Béla Kiss, Éva Schmidt, Judit Laszy, Katalin Sághy, Gyertyán, István, Zájer-Balázs, Mária, Gémesi, Larisza, Domány, György
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 01-10-2007 Elsevier
Subjects:	Animals Antipsychotic Antipsychotic Agents - chemical synthesis Antipsychotic Agents - metabolism Antipsychotic Agents - pharmacology Apomorphine - pharmacology Arylsulfonamides Avoidance Learning - drug effects Binding, Competitive - drug effects Biological and medical sciences Biological Availability Brain - metabolism Catalepsy - chemically induced Catecholaminergic system Cognition - drug effects Cognition enhancer Dopamine D3 and D2 ligands Humans Indicators and Reagents Male Maze Learning - drug effects Medical sciences Memory Disorders - chemically induced Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology Quantitative Structure-Activity Relationship Rats Rats, Wistar Receptors, Dopamine D2 - metabolism Receptors, Dopamine D3 - metabolism Stereotyped Behavior - drug effects Sulfonamides - chemical synthesis Sulfonamides - metabolism Sulfonamides - pharmacology Antipsychotic Arylsulfonamides Dopamine D3 and D2 ligands Cognition enhancer Nitrile Rat Nitrogen heterocycle Psychotropic Cognition D3 Dopamine receptor Structure activity relation Benzonitrile derivatives Antagonist Chemical synthesis Human Sulfonamide CNS stimulant Rodentia Benzene derivatives Oral administration Bioavailability In vitro In vivo Vertebrata Mammalia D2 Dopamine receptor Animal Affinity Piperazine derivatives Pharmacokinetics
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Summary:	Novel arylsulfonamides were identified as high-affinity dopamine D3 and D2 receptor ligands. Some derivatives were found to be active in antipsychotic tests in vivo. A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several members of this compound library were identified as high-affinity dopamine D3 and D2 receptor ligands. The most interesting representative, compound 2, showed potent antipsychotic behaviour coupled with a beneficial cognitive and EPS profile.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.08.015