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, 18 (4), 1331-5

Synthesis and SAR of Pyridazinone-Substituted Phenylalanine Amide alpha4 Integrin Antagonists

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Synthesis and SAR of Pyridazinone-Substituted Phenylalanine Amide alpha4 Integrin Antagonists

Yong Gong et al. Bioorg Med Chem Lett.

Abstract

Structural modification and cellular adhesion inhibition activities of pyridazinone-substituted phenylalanine amide alpha(4) integrin antagonists are described. Functionality requirements for the arylamide moiety and the carboxylic acid group were demonstrated. The study also revealed novel structure-activity relationships (SAR) for arylated pyridazinones. A correlation between bioavailability and permeability was also explored. A selected compound showed effectiveness in a mouse leukocytosis study.

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