1.
Bioorg Med Chem Lett
; 22(23): 7252-5, 2012 Dec 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23079519
RESUMO
Optimisation of a series of biaryl sulphonamides resulted in the identification of compound 14 [corrected] which demonstrated dose-dependent and strain-specific inhibition of monocyte recruitment in a thioglycollate-induced peritonitis model of inflammation. [Formula: see text]. [corrected].
Assuntos
Azóis/química , Receptores CCR2/antagonistas & inibidores , Sulfonamidas/química , Administração Oral , Animais , Azóis/síntese química , Azóis/farmacocinética , Inibidores das Enzimas do Citocromo P-450 , Sistema Enzimático do Citocromo P-450/metabolismo , Meia-Vida , Ligação Proteica , Ratos , Receptores CCR2/metabolismo , Relação Estrutura-Atividade , Sulfonamidas/síntese química , Sulfonamidas/farmacocinética
2.
Bioorg Med Chem Lett
; 20(13): 3961-4, 2010 Jul 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20627722
RESUMO
A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.