Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.

Article Details

Citation

Haubmann C, Hubner H, Gmeiner P

Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.

Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.

PubMed ID
10560741 [ View in PubMed
]
Abstract

Piperidinylpyrroles of type 3 were synthesized through a modified Paal-Knorr reaction. For the introduction of pyrrole-substituents high yielding transformations including Sonogashira cross-coupling reactions were utilized. Employment of the reagent TosMIC gave access to the regioisomeric oxazolyl derivatives 7 and 11 which showed the highest dopamine D4 receptor binding of the series investigated.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ClozapineDopamine D2 receptorKi (nM)28N/AN/ADetails
ClozapineDopamine D2 receptorKi (nM)41N/AN/ADetails
ClozapineDopamine D3 receptorKi (nM)960N/AN/ADetails
ClozapineDopamine D4 receptorKi (nM)16N/AN/ADetails