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N-Tetrahydrofuroyl-(l)-phenylalanine derivatives as potent VLA-4 antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 12:1497-1500
- Publication Year :
- 2002
- Publisher :
- Elsevier BV, 2002.
-
Abstract
- Given the proposed involvement of VLA-4 in inflammatory processes, a program to identify orally active VLA-4 antagonists was initiated. Herein, we report the discovery of a N -tetrahydrofuroyl-( l )-phenylalanine derivative ( 17 ) and related analogues as potent VLA-4 antagonists with good oral bioavailability.
- Subjects :
- Stereochemistry
Phenylalanine
Clinical Biochemistry
Administration, Oral
Biological Availability
Vascular Cell Adhesion Molecule-1
Pharmaceutical Science
Integrin alpha4beta1
Biochemistry
Chemical synthesis
Phenylalanine derivatives
Rats, Sprague-Dawley
Inhibitory Concentration 50
Structure-Activity Relationship
Pharmacokinetics
immune system diseases
Oral administration
hemic and lymphatic diseases
Drug Discovery
Animals
Furans
Molecular Biology
Sulfonamides
Binding Sites
Dose-Response Relationship, Drug
Chemistry
Organic Chemistry
Antagonist
VLA-4
hemic and immune systems
respiratory system
Macaca mulatta
In vitro
Rats
Bioavailability
Molecular Medicine
Half-Life
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 12
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....dc169a40d0f4e7ddf67123672405b6d9