N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists |
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| Authors: | Chen L Tilley J W Huang T N Miklowski D Trilles R Guthrie R W Luk K Hanglow A Rowan K Schwinge V Wolitzky B |
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| Affiliation: | Roche Research Center, Hoffmann-La Roche, Inc., Nutley, New Jersey 07110, USA. |
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| Abstract: | We have identified a series of low molecular weight (Mr < 500) N-acylphenylalanines that are effective inhibitors of the VCAM-VLA-4 interaction. Investigation of the SAR of the N-acyl moiety led to the identification of N-benzylpyroglutamyl derivatives as being particularly potent. |
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