| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1373037 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Structural modification and cellular adhesion inhibition activities of pyridazinone-substituted phenylalanine amide α4 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.
Graphical abstractStructure–activity relationships (SAR) within a series of pyridazinone-functionalized phenylalanine amide α4 integrin antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yong Gong, J. Kent Barbay, Edward S. Kimball, Rosemary J. Santulli, M. Carolyn Fisher, Alexey B. Dyatkin, Tamara A. Miskowski, Pamela J. Hornby, Wei He,