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Published on: January 22, 2019
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists
Li Chen1, Richard Trilles, Dorota Miklowski
1Roche Research Center, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, USA. li.chen@roche.com
Bioorganic & Medicinal Chemistry Letters
|June 1, 2002
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.
