1.
Bioorg Med Chem Lett
; 23(14): 4117-9, 2013 Jul 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23743283
RESUMEN
Mitsunobu reactions were employed to link t-butyl esters of α4 integrin inhibitors at each of the termini of a three-arm, 40 kDa, branched PEG. Cleavage of the t-butyl esters using HCO2H provided easily isolated PEG derivatives, which are potent α4 integrin inhibitors, and which achieve sustained levels and bioactivity in vivo, following subcutaneous administration to rats.
Asunto(s)
Integrina alfa4/química , Polietilenglicoles/química , Animales , Anticuerpos Monoclonales/química , Anticuerpos Monoclonales/inmunología , Anticuerpos Monoclonales/farmacocinética , Ésteres , Semivida , Humanos , Inyecciones Subcutáneas , Integrina alfa4/inmunología , Integrina alfa4/metabolismo , Células Jurkat , Ratas
2.
Bioorg Med Chem Lett
; 23(15): 4370-3, 2013 Aug 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-23777782
RESUMEN
A series of potent α4ß1/α4ß7 integrin inhibitors is reported, including an inhibitor 12d with remarkable oral exposure and efficacy in rat models of rheumatoid arthritis and Crohn's disease.