Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists |
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| Authors: | Chen Li Trilles Richard Miklowski Dorota Huang Tai-Nan Fry David Campbell Robert Rowan Karen Schwinge Virginia Tilley Jefferson W |
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| Institution: | Roche Research Center, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, USA. li.chen@roche.com |
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| Abstract: | A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists characterized by the N-(alpha-phenylcyclopentanoyl- and the N-(2,6-dimethylbenzoyl)-derivatives 60 and 64. |
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