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Dehydrophenylalanine derivatives as VLA-4 integrin antagonists |
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| Authors: | Porter John R Archibald Sarah C Brown Julien A Childs Kirstie Critchley David Head John C Parton Ted A H Robinson Martyn K Shock Anthony Taylor Richard J Warrellow Graham J |
| Affiliation: | Department of Medicinal Chemistry, Celltech R&D Ltd, 216 Bath Road, Slough SL1 4EN, UK. john.porter@celltechgroup.com |
| 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. |
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