Author/Authors :
John R. Porter، نويسنده , , Sarah C. Archibald، نويسنده , , Julien A. Brown، نويسنده , , Kirstie Childs، نويسنده , , David Critchley، نويسنده , , John C. Head، نويسنده , , Ted A. H. Parton، نويسنده , , Martyn K. Robinson، نويسنده , , Anthony Shock، نويسنده , , Richard J. Taylor، نويسنده , , Graham J. Warrellow، نويسنده ,
Abstract :
We describe a series of dehydrophenylalanine derivatives where the Z isomers are potent VLA-4 antagonists but are subject to rapid biliary clearance and the E isomers have poor activity but have a slower rate of clearance. These configurationally constrained molecules have led to the design of a novel class of benzodiazepine VLA-4 antagonists.
