Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists

Autor:	Richard A. Mumford, William K. Hagmann, Karen Owens, Plato A. Magriotis, Gail Van Riper, David N. Young, Ermengilda McCauley, Sharon Tong, Linus S. Lin, Usha Kidambi, Stephen E. deLaszlo, Ralph A. Stearns, John A. Schmidt, Adria Colletti, Yohannes Teffera, Kathryn A. Lyons, Malcolm MacCoss, Linda A. Egger, Dorothy Levorse, Thomas J. Lanza, Ihor E. Kopka, Stella H. Vincent, Sander G. Mills
Rok vydání:	2002
Předmět:	Metabolic Clearance Rate Stereochemistry Clinical Biochemistry Administration Oral Biological Availability Vascular Cell Adhesion Molecule-1 Pharmaceutical Science Peptide Integrin alpha4beta1 Biochemistry Chemical synthesis Inhibitory Concentration 50 Jurkat Cells Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Potency Molecular Biology chemistry.chemical_classification Alanine Dipeptide Organic Chemistry Blood proteins In vitro Sulfonamide Bioavailability chemistry Molecular Medicine Propionates Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 12:2415-2418
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(02)00460-2
Popis:	A series of substituted N-(3,5-dichlorobenzenesulfonyl)-( l )-prolyl- and ( l )-azetidyl-β-biaryl β-alanine derivatives was prepared as selective and potent VLA-4 antagonists. The 2,6-dioxygenated biaryl substitution pattern is important for optimizing potency. Oral bioavailability was variable and may be a result of binding to circulating plasma proteins.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afd9969200d9a04b695d0ef385ea944b https://doi.org/10.1016/s0960-894x(02)00460-2 Zobrazit plný text záznamu Full Text from ScienceDirect