2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands.
The phenylpiperazinylmethyl substituted pyrrolylmethylenemalononitriles of type 3 and 4 were synthesized and evaluated as strong and selective dopamine D4 receptor ligands.
Haubmann
C
C
Institut für Pharmazie und Lebensmittelchemie, Universität Erlangen - Nürnberg, Erlangen, Germany.
Hübner
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H
Gmeiner
P
P
D000818:Animals; D014150:Antipsychotic Agents / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D016466:CHO Cells / Q000187:drug effects / Q000378:metabolism; D002417:Cattle; D003024:Clozapine / Q000378:metabolism; D006224:Cricetinae; D006801:Humans; D007536:Isomerism; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D009570:Nitriles / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D010879:Piperazines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D017447:Receptors, Dopamine D1 / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
D014150:Antipsychotic Agents; C493599:DRD4 protein, human; D008024:Ligands; D009570:Nitriles; D010879:Piperazines; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D050638:Receptors, Dopamine D4; D003024:Clozapine