Sulphonamide-based small molecule VLA-4 antagonists

The discovery of a sulphonamide by-product with VLA-4 antagonistic activity led to a series of potent, small molecule VLA-4 antagonists. Synthesis, SAR and in vivo evaluation of the selected compound will be presented.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (21), p.3875-3878
Hauptverfasser:	STASIAK, Marcin, MEHLIN, Christopher, BONI, Erica, VAISAR, Tomas, LITTLE, Thomas, KIM, Hwa-Ok, QABAR, Maher
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Asthma - drug therapy Asthma - pathology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Adhesion - drug effects Cell Line Cell Movement - drug effects Eosinophils - drug effects Female Half-Life Indicators and Reagents Integrin alpha4beta1 - antagonists & inhibitors Leukocytes - drug effects Macaca fascicularis Medical sciences Mice Mice, Inbred BALB C Ovalbumin - immunology Pharmacology. Drug treatments Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - pharmacology
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Beschreibung
Zusammenfassung:	The discovery of a sulphonamide by-product with VLA-4 antagonistic activity led to a series of potent, small molecule VLA-4 antagonists. Synthesis, SAR and in vivo evaluation of the selected compound will be presented.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00760-1