Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists

Authors
Tilley, JW Kaplan, G Rowan, K Schwinge, V Wolitzky, B
Citation
Jw. Tilley et al., Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists, BIOORG MED, 11(1), 2001, pp. 1-4
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
1
Year of publication
2001
Pages
1 - 4
Database
ISI
SICI code
0960-894X(20010108)11:1<1:IALDON>2.0.ZU;2-B
Abstract
A series of imides and lactams derived from 4-amino-N-benzylpyroglutamyl-L- phenylalanine was prepared and evaluated for activity as VCAM/VLA-4 antagon ists. Imides were more potent than the corresponding lactams; several had s ubnanomolar IC(50)s in an ELISA based assay and were also highly effective at blocking VLA-4 expressing Ramos cell binding to VCAM coated plates. (C) 2000 Elsevier Science Ltd. All rights reserved.