Peer-reviewed veterinary case report
Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
- Journal:
- Bioorganic & medicinal chemistry
- Year:
- 2008
- Authors:
- Muro, Fumihito et al.
- Affiliation:
- Medicinal Chemistry Research Laboratories II · Japan
Abstract
Optimization of benzoic acid derivatives by introducing substituents into the diphenyl urea moiety led to the identification of compound 20l as a potent VLA-4 antagonist. Compound 20l inhibited eosinophil infiltration into bronchial alveolar lavage fluid in a murine asthma model by oral dosing and its efficacy was comparable to anti-mouse alpha4 antibody (R1-2). Furthermore, this compound significantly blocked bronchial hyper-responsiveness in the model.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/18952443/