Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands.
Article Details
- CitationCopy to clipboard
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
Drug Target Property Measurement pH Temperature (°C) Clozapine Dopamine D2 receptor Ki (nM) 28 N/A N/A Details Clozapine Dopamine D2 receptor Ki (nM) 41 N/A N/A Details Clozapine Dopamine D3 receptor Ki (nM) 960 N/A N/A Details Clozapine Dopamine D4 receptor Ki (nM) 16 N/A N/A Details