title: New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
abstract: 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.
authors.affiliation: Global Chemical Sciences Department, Wyeth-Ayerst Research Laboratories, Princeton NJ 08543-8000, USA.
authors.forename: R E
authors.initials: RE
authors.lastname: Mewshaw
authors.forename: J A
authors.initials: JA
authors.lastname: Nelson
authors.forename: U S
authors.initials: US
authors.lastname: Shah
authors.forename: X
authors.initials: X
authors.lastname: Shi
authors.forename: H
authors.initials: H
authors.lastname: Mazandarani
authors.forename: J
authors.initials: J
authors.lastname: Coupet
authors.forename: K
authors.initials: K
authors.lastname: Marquis
authors.forename: J A
authors.initials: JA
authors.lastname: Brennan
authors.forename: T H
authors.initials: TH
authors.lastname: Andree
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015259:Dopamine Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D017448:Receptors, Dopamine D2 / Q000187:drug effects*
chemical_list: D001562:Benzimidazoles; D015259:Dopamine Agents; D017448:Receptors, Dopamine D2