Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists

Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists

A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists characterized by the N-(α-phenylcyclopentanoyl- a...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2002-06, Vol.12 (12), p.1679-1682
Hauptverfasser: Chen, Li, Trilles, Richard, Miklowski, Dorota, Huang, Tai-Nan, Fry, David, Campbell, Robert, Rowan, Karen, Schwinge, Virginia, Tilley, Jefferson W.
Format: Artikel
Sprache:eng
Schlagworte:
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cell Line
Immunomodulators
Integrin alpha4beta1 - antagonists & inhibitors
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Phenylalanine - chemistry
Phenylalanine - pharmacology
Vascular Cell Adhesion Molecule-1 - drug effects
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Zusammenfassung:A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists characterized by the N-(α-phenylcyclopentanoyl- and the N-(2,6-dimethylbenzoyl)-derivatives 60 and 64. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00201-9