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.
Stasiak
Marcin
M
Molecumetics, 2023 120th Avenue N E., Bellevue, WA 98005, USA.
Mehlin
Christopher
C
Boni
Erica
E
Vaisar
Tomas
T
Little
Thomas
T
Kim
Hwa-Ok
HO
Qabar
Maher
M
D000818:Animals; D001249:Asthma / Q000188:drug therapy / Q000473:pathology; D002448:Cell Adhesion / Q000187:drug effects; D002460:Cell Line; D002465:Cell Movement / Q000187:drug effects; D004804:Eosinophils / Q000187:drug effects; D005260:Female; D006207:Half-Life; D007202:Indicators and Reagents; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors*; D007962:Leukocytes / Q000187:drug effects; D008252:Macaca fascicularis; D051379:Mice; D008807:Mice, Inbred BALB C; D010047:Ovalbumin / Q000276:immunology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
D007202:Indicators and Reagents; D039041:Integrin alpha4beta1; D013449:Sulfonamides; D010047:Ovalbumin