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

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Einsiedel J, Thomas C, Hubner H, Gmeiner P

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

Bioorg Med Chem Lett. 2000 Sep 4;10(17):2041-4.

PubMed ID
10987445 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ClozapineDopamine D2 receptorKi (nM)39N/AN/ADetails
ClozapineDopamine D2 receptorKi (nM)28N/AN/ADetails
ClozapineDopamine D3 receptorKi (nM)960N/AN/ADetails
ClozapineDopamine D4 receptorKi (nM)16N/AN/ADetails
SulpirideDopamine D2 receptorKi (nM)120N/AN/ADetails
SulpirideDopamine D2 receptorKi (nM)51N/AN/ADetails
SulpirideDopamine D3 receptorKi (nM)88N/AN/ADetails