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Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha(4) integrin antagonists
Journal article   Peer reviewed

Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha(4) integrin antagonists

Yong Gong, J. Kent Barbay, Edward S. Kimball, Rosemary J. Santulli, M. Carolyn Fisher, Alexey B. Dyatkin, Tamara A. Miskowski, Pamela J. Hornby and Wei He
Bioorganic & medicinal chemistry letters, v 18(4), pp 1331-1335
15 Feb 2008
PMID: 18226905
url
https://doi.org/10.7270/q2td9z6wView
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Abstract

Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
Structural modi. cation 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. (c) 2008 Elsevier Ltd. All rights reserved.

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Web of Science research areas
Chemistry, Medicinal
Chemistry, Organic
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