1.
Bioorg Med Chem Lett
; 16(10): 2724-8, 2006 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16540318
RESUMO
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.
Assuntos
Pirimidinas/farmacologia , Receptores de Interleucina-8B/antagonistas & inibidores , Administração Oral , Animais , Células CHO , Cricetinae , Humanos , Testes de Sensibilidade Microbiana , Pirimidinas/administração & dosagem , Pirimidinas/farmacocinética , Proteínas Recombinantes/antagonistas & inibidores
2.
Bioorg Med Chem Lett
; 14(2): 545-8, 2004 Jan 19.
Artigo
em Inglês
| MEDLINE
| ID: mdl-14698200
RESUMO
Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors.