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Peer-reviewed veterinary case report

Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2011
Authors:
Semko, Christopher M et al.
Affiliation:
Elan Pharmaceuticals · United States

Abstract

A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave 14, a very potent VLA-4 inhibitor which is orally active in a sheep asthma model.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/21316228/