N-aryl-prolyl-dipeptides as potent antagonists of VLA-4

TM Kamenecka, T Lanza Jr, SE de Laszlo, B Li… - Bioorganic & medicinal …, 2002 - Elsevier
TM Kamenecka, T Lanza Jr, SE de Laszlo, B Li, ED McCauley, G Van Riper, LA Egger…
Bioorganic & medicinal chemistry letters, 2002Elsevier
The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as
small molecule VLA-4 antagonists is described. Potency against VLA-4 and α4β7 and rat
pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-
prolyl-dipeptide analogues.
The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and α4β7 and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.
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