N-Acyl phenylalanine analogues as potent small molecule VLA-4 antagonists

We have identified a series of low molecular weight (Mr < 500) N-acylphenylalanines that are effective inhibitors of the VCAM-VLA-4 interaction. Investigation of the SAR of the N-acyl moiety led to the identification of N-benzylpyroglutamyl derivatives as being particularly potent.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.725-727
Hauptverfasser:	LI CHEN, TILLEY, J. W, WOLITZKY, B, HUANG, T.-N, MIKLOWSKI, D, TRILLES, R, GUTHRIE, R. W, KIN LUK, HANGLOW, A, ROWAN, K, SCHWINGE, V
Format:	Artikel
Sprache:	eng
Schlagworte:	Acylation Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Integrin alpha4beta1 Integrins - antagonists & inhibitors Medical sciences Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - pharmacology Receptors, Lymphocyte Homing - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	We have identified a series of low molecular weight (Mr < 500) N-acylphenylalanines that are effective inhibitors of the VCAM-VLA-4 interaction. Investigation of the SAR of the N-acyl moiety led to the identification of N-benzylpyroglutamyl derivatives as being particularly potent.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00088-3