Peer-reviewed veterinary case report
4-(Pyrrolidinyl)methoxybenzoic acid derivatives as a potent, orally active VLA-4 antagonist.
- Journal:
- Chemical & pharmaceutical bulletin
- Year:
- 2006
- Authors:
- Chiba, Jun et al.
- Affiliation:
- Medicinal Chemistry Research Laboratory · Japan
Abstract
A novel series of benzoic acid derivatives as VLA-4 antagonists were synthesized. Optimization, focusing on activity and lipophilicity needed for cell permeability, resulted in the identification of 15b and 15e with good activity (IC50 = 1.6 nM each) and moderate lipophilicity (Log D = 2.0, 1.8). Furthermore, 15e demonstrated efficacy in murine asthma model by an oral dose of 30 mg/kg.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/17077548/