N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists
B Li, SE de Laszlo, TM Kamenecka, IE Kopka… - Bioorganic & medicinal …, 2002 - Elsevier
B Li, SE de Laszlo, TM Kamenecka, IE Kopka, PL Durette, T Lanza Jr, M MacCoss, S Tong…
Bioorganic & medicinal chemistry letters, 2002•ElsevierA series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4
antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further
optimization led to several highly potent compounds (IC50< 1 nM). Evaluation of rat
pharmacokinetic revealed generally high clearance.
antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further
optimization led to several highly potent compounds (IC50< 1 nM). Evaluation of rat
pharmacokinetic revealed generally high clearance.
A series of potent N-(aralkyl-, arylcycloalkyl-, and heteroaryl-acyl)-4-biphenylalanine VLA-4 antagonists was prepared by rapid analogue methods using solid-phase chemistry. Further optimization led to several highly potent compounds (IC50 <1 nM). Evaluation of rat pharmacokinetic revealed generally high clearance.
Elsevier