Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands
Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands
Citació
- Ortega R, Raviña E, Masaguer CF, Areias F, Brea J, Loza MI et al. Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands. Bioorg Med Chem Lett. 2009;19(6):1773-8. DOI: 10.1016/j.bmcl.2009.01.067
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Resum
A series of new benzolactam derivatives was synthesized and the derivatives were evaluated for their/naffinities at the dopamine D1, D2, and D3 receptors. Some of these compounds showed high D2 and/or/nD3 affinity and selectivity over the D1 receptor. The SAR study of these compounds revealed structural/ncharacteristics that decisively influenced their D2 and D3 affinities. Structural models of the complexes/nbetween some of the most representative compounds of this series and the D2 and D3 receptors were/nobtained with the aim of rationalizing the observed experimental results. Moreover, selected compounds/nshowed moderate binding affinity on 5-HT2A which could contribute to reducing the occurrence of extrapyramidal/nside effects as potential antipsychotics.