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Published on: June 23, 2019
Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists
Yong Gong1, J Kent Barbay, Edward S Kimball
1Johnson & Johnson Pharmaceutical Research & Development, L.L.C., Welsh & McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA.
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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