Add time:07/25/2019         Source:sciencedirect.com

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 α4 antibody (R1-2). Furthermore, this compound significantly blocked bronchial hyper-responsiveness in the model.

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