1.
Bioorg Med Chem Lett
; 22(21): 6694-9, 2012 Nov 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23021991
RESUMO
The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with excellent selectivity over activity at hERG and outstanding pharmacokinetics in preclinical species.
Assuntos
Descoberta de Drogas , Piperidinas/química , Piperidinas/farmacocinética , Receptores CCR3/antagonistas & inibidores , Animais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ratos
2.
J Med Chem
; 50(24): 5882-5, 2007 Nov 29.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17963373
RESUMO
A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.