Imidazo[1,2-a]pyrimidines as functionally selective GABAA ligands

• DOI: 10.1016/j.bmcl.2005.11.112
• Publication Date: 2006-01-07T12:22:01Z
• Authors: Wesley P. Blackaby; John R. Atack; Frances Bromidge; José L. Castro; Simon C. Goodacre; David J. Hallett; Richard T. Lewis; George R. Marshall; Andrew Pike; Alison J. Smith; Leslie J. Street; David F.D. Tatter...; Keith A. Wafford
• Keywords: Structure-Activity Relationship; Pyrimidines; Molecular Structure; Imidazoles; Ligands; Receptors, GABA-A; Sensitivity and Specificity; 01 natural sciences; Substrate Specificity; 0104 chemical sciences; 3. Good health

Imidazo[1,2-a]pyrimidines are GABA(A) receptor benzodiazepine binding site ligands which can exhibit functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimize this functional selectivity are described.