Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands

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 Tattersall; Keith A Wafford

doi:10.1016/j.bmcl.2005.11.112

Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1175-9. doi: 10.1016/j.bmcl.2005.11.112. Epub 2006 Jan 6.

Authors

Wesley P Blackaby¹, 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 Tattersall, Keith A Wafford

Affiliation

¹ Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. Wesley_Blackaby@merck.com

PMID: 16406613
DOI: 10.1016/j.bmcl.2005.11.112

Abstract

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.

MeSH terms

Imidazoles / chemistry*
Imidazoles / metabolism*
Ligands
Molecular Structure
Pyrimidines / chemical synthesis
Pyrimidines / chemistry*
Pyrimidines / metabolism*
Receptors, GABA-A / metabolism*
Sensitivity and Specificity
Structure-Activity Relationship
Substrate Specificity

Substances

Imidazoles
Ligands
Pyrimidines
Receptors, GABA-A
imidazole