Synthesis and binding affinity of new 1,4-disubstituted triazoles as potential dopamine D3 receptor ligands |
| |
| Authors: | Ignacio Insua Mario Alvarado Christian F. Masaguer Alba Iglesias José Brea María I. Loza Laura Carro |
| |
| Affiliation: | 1. Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, E-15782 Santiago de Compostela, Spain;2. Grupo de Investigación en Compuestos Heterocíclicos, Semillero de Investigación en Química Médica, Facultad de Ciencias Básicas, Universidad del Atlántico, A.A. 1890 Barranquilla, Colombia;3. Departamento de Farmacología, Facultad de Farmacia, Universidad de Santiago de Compostela, E-15782 Santiago de Compostela, Spain |
| |
| Abstract: | A series of new 1,4-disubstituted triazoles was prepared from appropriate arylacetylenes and aminoalkylazides using click chemistry methodology. These compounds were evaluated as potential ligands on several subtypes of dopamine receptors in in vitro competition assays, showing high affinity for dopamine D3 receptors, lower affinity for D2 and D4, and no affinity for the D1 receptors. Compound 18 displayed the highest affinity at the D3 receptor with a Ki value of 2.7 nM, selectivity over D2 (70-fold) and D4 (200-fold), and behaviour as a competitive antagonist in the low nanomolar range. |
| |
| Keywords: | 1,2,3-Triazoles Synthesis Click chemistry Microwaves Binding assays Dopamine receptors |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
