Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template

John Spencer; John Gaffen; Eric Griffin; Elaine A Harper; Ian D Linney; Iain M McDonald; Sonia P Roberts; Mark E Shaxted; Trushar Adatia; Alan Bashall

doi:10.1016/j.bmc.2007.12.047

Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template

Bioorg Med Chem. 2008 Mar 15;16(6):2974-83. doi: 10.1016/j.bmc.2007.12.047. Epub 2007 Dec 25.

Authors

John Spencer¹, John Gaffen, Eric Griffin, Elaine A Harper, Ian D Linney, Iain M McDonald, Sonia P Roberts, Mark E Shaxted, Trushar Adatia, Alan Bashall

Affiliation

¹ James Black Foundation, 68 Half Moon Lane, Dulwich, London SE24 9JE, UK.

PMID: 18289857
DOI: 10.1016/j.bmc.2007.12.047

Abstract

Novel, achiral 1H-1,3,5-benzotriazepine-2,4(3H,5H)-diones have been prepared and structurally characterized. These compounds are potent CCK(2) receptor antagonists that display a high degree of selectivity over CCK(1) receptors.

MeSH terms

Animals
Benzazepines / chemistry
Benzazepines / pharmacology
Humans
Protein Binding
Receptor, Cholecystokinin B / antagonists & inhibitors*
Structure-Activity Relationship
Triazines / chemistry*
Triazines / pharmacology*

Substances

Benzazepines
Receptor, Cholecystokinin B
Triazines