1.
Chem Pharm Bull (Tokyo)
; 54(11): 1515-29, 2006 Nov.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17077548
RESUMO
A novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50 = 1.6 nM each) and moderate lipophilicity (Log D = 2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.