Journal of medicinal chemistry, 2010-10, Vol.53 (19), p.7129-7139
2010
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Details
- Autor(en) / Beteiligte
- Titel
- Exploration of the Amine Terminus in a Novel Series of 1,2,4-Triazolo-3-yl-azabicyclo[3.1.0]hexanes as Selective Dopamine D3 Receptor Antagonists
- Ist Teil von
- Journal of medicinal chemistry, 2010-10, Vol.53 (19), p.7129-7139
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2010
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes with high affinity and selectivity for the DA D3 receptor and excellent pharmacokinetic profiles was recently reported. We also recently discussed the role of the linker associated with the triazole moiety. In this manuscript, we are reporting a detailed exploration of the region of the receptor interacting with the amine terminus of the scaffold wherein SAR and developability data associated with these novel templates was undertaken.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm100832dTitel-ID: cdi_proquest_miscellaneous_757175917
- Format
- –
- Schlagworte
- Animals, Azabicyclo Compounds - chemical synthesis, Azabicyclo Compounds - chemistry, Azabicyclo Compounds - pharmacology, Catalytic Domain, CHO Cells, Cricetinae, Cricetulus, Humans, In Vitro Techniques, Microsomes, Liver - metabolism, Models, Molecular, Radioligand Assay, Rats, Receptors, Dopamine D3 - antagonists & inhibitors, Structure-Activity Relationship, Triazoles - chemical synthesis, Triazoles - chemistry, Triazoles - pharmacology