Abstract
Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K(i)high=0.95nM). Mitogenesis experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from alpha-amino acids.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Biochemistry / methods
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CHO Cells
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Cattle
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Clozapine / pharmacology
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Cricetinae
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Cysteine / chemistry
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Dopamine Antagonists / metabolism
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Drug Design
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Humans
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In Vitro Techniques
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Indoles / chemistry*
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Indoles / metabolism
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Indoles / pharmacology*
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Quinpirole / pharmacology
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Receptors, Dopamine D2 / agonists*
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Receptors, Dopamine D2 / metabolism
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Receptors, Dopamine D4
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Serine / chemistry
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Spiperone / metabolism
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Stereoisomerism
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Structure-Activity Relationship
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Threonine / chemistry
Substances
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DRD4 protein, human
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Dopamine Antagonists
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FAUC 179
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Indoles
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Receptors, Dopamine D2
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Receptors, Dopamine D4
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Quinpirole
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Threonine
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Serine
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Spiperone
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Clozapine
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Cysteine