Sulphonamide-based small molecule VLA-4 antagonists

Marcin Stasiak; Christopher Mehlin; Erica Boni; Tomas Vaisar; Thomas Little; Hwa-Ok Kim; Maher Qabar

doi:10.1016/s0960-894x(03)00760-1

Sulphonamide-based small molecule VLA-4 antagonists

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3875-8. doi: 10.1016/s0960-894x(03)00760-1.

Authors

Marcin Stasiak¹, Christopher Mehlin, Erica Boni, Tomas Vaisar, Thomas Little, Hwa-Ok Kim, Maher Qabar

Affiliation

¹ Molecumetics, 2023 120th Avenue N E., Bellevue, WA 98005, USA.

PMID: 14552799
DOI: 10.1016/s0960-894x(03)00760-1

Abstract

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.

MeSH terms

Animals
Asthma / drug therapy
Asthma / pathology
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
Mice
Mice, Inbred BALB C
Ovalbumin / immunology
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology*

Substances

Indicators and Reagents
Integrin alpha4beta1
Sulfonamides
Ovalbumin