| Autor: |
Micheli F; Neurosciences Centre of Excellence, GlaxoSmithKline Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy. fabrizio.micheli@aptuit.com, Arista L, Bertani B, Braggio S, Capelli AM, Cremonesi S, Di-Fabio R, Gelardi G, Gentile G, Marchioro C, Pasquarello A, Provera S, Tedesco G, Tarsi L, Terreni S, Worby A, Heidbreder C |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2010 Oct 14; Vol. 53 (19), pp. 7129-39. |
| DOI: |
10.1021/jm100832d |
| Abstrakt: |
A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes with high affinity and selectivity for the DA D(3) 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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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