N-Benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists

A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA assay and low-microM activity in a cell based assay.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.729-733
Hauptverfasser:	LI CHEN, TILLEY, J. W, WOLITZKY, B, ROWAN, K, GUTHRIE, R. W, MENNONA, F, HUANG, T.-N, KAPLAN, G, TRILLES, R, MIKLOWSKI, D, HUBY, N, SCHWINGE, V
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Enzyme-Linked Immunosorbent Assay Humans Integrin alpha4beta1 Integrins - antagonists & inhibitors Medical sciences Pharmacology. Drug treatments Phenylalanine - analogs & derivatives Phenylalanine - chemistry Phenylalanine - pharmacology Receptors, Lymphocyte Homing - antagonists & inhibitors Recombinant Proteins - antagonists & inhibitors Structure-Activity Relationship Vascular Cell Adhesion Molecule-1 - drug effects
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A series of N-(N-benzylpyroglutamyl)-4-substituted-L-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. Analogues substituted by electron deficient benzoylamino groups bearing bulky ortho substituents had low-nM potency in an ELISA assay and low-microM activity in a cell based assay.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00089-5