N-Cycloalkanoyl-l-Phenylalanine Derivatives as VCAM/VLA-4 Antagonists

Autor:	Louis M. Renzetti, Li Chen, Karen Rowan, Allen Sheffron, Tai-Nan Huang, Jian Ping Lou, Jefferson Wright Tilley, Kenneth G. Hull, Virginia Schwinge, Gerry Kaplan, Achyutharao Sidduri, Robert M. Campbell, Robert William Guthrie, Nicholas John Silvester Huby
Rok vydání:	2002
Předmět:	medicine.drug_class Stereochemistry Phenylalanine Clinical Biochemistry Vascular Cell Adhesion Molecule-1 Pharmaceutical Science Carboxamide Integrin alpha4beta1 Crystallography X-Ray Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Humans Molecule Molecular Biology Alkyl chemistry.chemical_classification Molecular Structure Organic Chemistry Antagonist Cycloparaffins In vitro Cycloalkane chemistry Molecular Medicine Lead compound Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 12:2475-2478
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(02)00386-4
Popis:	A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 antagonists. The data are consistent with a model of these compounds in which these alkanoylphenylalanines reside in a compact gauche (-) bioactive conformation.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53da7a5e27aecfcea2db394b82b8d572 https://doi.org/10.1016/s0960-894x(02)00386-4 Zobrazit plný text záznamu Full Text from ScienceDirect