1.
Bioorg Med Chem Lett
; 20(3): 1173-6, 2010 Feb 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20022493
RESUMO
A variety of N-linked tertiary amines and heteroarylamines were examined at the 4-position of sulfonylated proline dipeptides in order to improve VLA-4 receptor off-rates and overcome the issue of CYP3A4 time-dependent inhibition of ester prodrugs. A tight-binding inhibitor 5j with a long off-rate provided sustained receptor occupancy despite poor oral pharmacokinetics.