Part 1: N-alkylated glycines as potent α2δ ligands

Lisa R Thompson; David C Blakemore; Delphine Brugier; Justin S Bryans; Wai-Lam A Chu; Graham N Maw; Cedric Poinsard; David J Rawson; Andrew N Warren

doi:10.1016/j.bmcl.2011.04.045

Part 1: N-alkylated glycines as potent α2δ ligands

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3764-6. doi: 10.1016/j.bmcl.2011.04.045. Epub 2011 Apr 30.

Authors

Lisa R Thompson¹, David C Blakemore, Delphine Brugier, Justin S Bryans, Wai-Lam A Chu, Graham N Maw, Cedric Poinsard, David J Rawson, Andrew N Warren

Affiliation

¹ Sandwich Laboratories, Pfizer Global Research and Development, Sandwich, Kent, UK.

PMID: 21601457
DOI: 10.1016/j.bmcl.2011.04.045

Abstract

A new series of glycine-derived ligands of the α(2)δ subunit of voltage gated calcium channels is described. Several novel compounds (7) based on (6) were prepared that possessed a potency <100 nM in the α(2)δ binding assay.

MeSH terms

Alkylation
Calcium Channels / drug effects*
Glycine / chemical synthesis*
Glycine / chemistry
Glycine / pharmacology
Inhibitory Concentration 50
Ligands*
Molecular Structure
Protein Subunits / chemistry
Structure-Activity Relationship

Substances

Calcium Channels
Ligands
Protein Subunits
Glycine