Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles

J Einsiedel; C Thomas; H Hübner; P Gmeiner

doi:10.1016/s0960-894x(00)00405-4

Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles

Bioorg Med Chem Lett. 2000 Sep 4;10(17):2041-4. doi: 10.1016/s0960-894x(00)00405-4.

Authors

J Einsiedel¹, C Thomas, H Hübner, P Gmeiner

Affiliation

¹ Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Erlangen, Germany.

PMID: 10987445
DOI: 10.1016/s0960-894x(00)00405-4

Abstract

Conformationally restricted benzamide bioisosteres were investigated when the aminomethylpyrrolidine derivative 4o proved D3 as well as D4 binding properties which were comparable to those of the atypical neuroleptics sulpiride and clozapine, respectively.

MeSH terms

Antipsychotic Agents / chemical synthesis*
Benzamides / chemical synthesis*
Benzamides / metabolism
Humans
Oxazoles / chemical synthesis*
Oxazoles / metabolism
Receptors, Dopamine / metabolism*
Structure-Activity Relationship
Thiazoles / chemical synthesis*
Thiazoles / metabolism

Substances

Antipsychotic Agents
Benzamides
Oxazoles
Receptors, Dopamine
Thiazoles