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N-aryl-prolyl-dipeptides as potent antagonists of VLA-4
Theodore M Kamenecka1, Thomas Lanza, Stephen E de Laszlo
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. theodore_kamenecka@merck.com
Bioorganic & Medicinal Chemistry Letters
|July 20, 2002
Abstract:
The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.