Discovery and evaluation of terephthalic acid derivatives as potent alpha4beta1 integrin antagonists

Discovery and evaluation of terephthalic acid derivatives as potent alpha4beta1 integrin antagonists

Terephthalic acid based derivatives containing beta- and gamma-amino acid residues were prepared as antagonists of the leukocyte cell adhesion process that is mediated through the interaction of the very late antigen 4 (VLA-4) and the vascular cell adhesion molecule 1 (VCAM-1). The compounds 2, 10-1...

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Veröffentlicht in:Journal of enzyme inhibition and medicinal chemistry 2003-08, Vol.18 (4), p.309-312
Hauptverfasser: Müller, Gerhard, Albers, Markus, Hessler, Gerhard, Lehmann, Thomas E, Okigami, Hiromi, Tajimi, Masaomi, Bacon, Kevin, Rölle, Thomas
Format: Artikel
Sprache:eng
Schlagworte:
Amides - chemistry
Cell Adhesion - drug effects
Humans
Integrin alpha4beta1 - antagonists & inhibitors
Phthalic Acids - chemistry
Phthalic Acids - pharmacology
Urea - chemistry
Vascular Cell Adhesion Molecule-1 - chemistry
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Zusammenfassung:Terephthalic acid based derivatives containing beta- and gamma-amino acid residues were prepared as antagonists of the leukocyte cell adhesion process that is mediated through the interaction of the very late antigen 4 (VLA-4) and the vascular cell adhesion molecule 1 (VCAM-1). The compounds 2, 10-12, 14, and 16-17 inhibited the adhesion in a cell based assay in the low and sub micromolar range.
ISSN:1475-6366