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Bioorg Med Chem Lett. 2008 Feb 15;18(4):1331-5. doi: 10.1016/j.bmcl.2008.01.022. Epub 2008 Jan 11.

Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists.

Author information

1
Johnson & 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.

PMID:
18226905
DOI:
10.1016/j.bmcl.2008.01.022
[Indexed for MEDLINE]

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