New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template

The synthesis of several bioisosteric analogs based on the 3-OH-phenoxyethylamine dopamine D2 agonist template (i.e., 3) is described. The benzimidazol-2-ones and benzthioimidazol-2-ones (7-10) and 2-trifluoromethyl-benzimidazole (13) were observed to have excellent affinity for the D2 receptor.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2593-2598
Hauptverfasser:	MEWSHAW, R. E, NELSON, J. A, SHAH, U. S, XIAOJIE SHI, MAZANDARANI, H, COUPET, J, MARQUIS, K, BRENNAN, J. A, ANDREE, T. H
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Catecholaminergic system Dopamine Agents - chemical synthesis Dopamine Agents - chemistry Dopamine Agents - pharmacology Medical sciences Mice Motor Activity - drug effects Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptors, Dopamine D2 - drug effects
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Beschreibung
Zusammenfassung:	The synthesis of several bioisosteric analogs based on the 3-OH-phenoxyethylamine dopamine D2 agonist template (i.e., 3) is described. The benzimidazol-2-ones and benzthioimidazol-2-ones (7-10) and 2-trifluoromethyl-benzimidazole (13) were observed to have excellent affinity for the D2 receptor.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00434-5