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

Bioorg Med Chem Lett

Global Chemical Sciences Department, Wyeth-Ayerst Research Laboratories, Princeton NJ 08543-8000, USA.

Published: September 1999

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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http://dx.doi.org/10.1016/s0960-894x(99)00434-5DOI Listing

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