1.
Bioorg Med Chem
; 16(6): 2974-83, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18289857
RESUMO
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.
Assuntos
Receptor de Colecistocinina B/antagonistas & inibidores , Triazinas/química , Triazinas/farmacologia , Animais , Benzazepinas/química , Benzazepinas/farmacologia , Humanos , Ligação Proteica , Relação Estrutura-Atividade
2.
J Med Chem
; 49(7): 2253-61, 2006 Apr 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16570921
RESUMO
A series of 1,3,4-benzotriazepine-based CCK(2) antagonists have been devised by consideration of the structural features that govern CCK receptor affinity and the receptor subtype selectivity of 1,4-benzodiazepine-based CCK(2) antagonists. In contrast to the latter compounds, these novel 1,3,4-benzotriazepines are achiral, yet they display similar affinity for CCK(2) receptors to the earlier molecules and are highly selective over CCK(1) receptors.