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Bioorg Med Chem Lett. 2002 Sep 2;12(17):2479-82.

N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.

Author information

1
Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. achyutharao.sidduri@roche.com

Abstract

A series of N-benzoyl-4-[(2,6-dichlorobenzoyl)amino]-L-phenylalanine derivatives was prepared in order to optimize the substitution on the N-benzoyl moiety for VCAM/VLA-4 antagonist activity. Disubstitution in the 2- and 6-positions is favored and a range of small alkyl and halogen are tolerated. A model of the bioactive conformation of these compounds is proposed.

PMID:
12161162
DOI:
10.1016/s0960-894x(02)00387-6
[Indexed for MEDLINE]

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