Literature DB >> 11140722

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

J W Tilley1, G Kaplan, K Rowan, V Schwinge, B Wolitzky.   

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 antagonists. Imides were more potent than the corresponding lactams; several had subnanomolar IC50s in an ELISA based assay and were also highly effective at blocking VLA-4 expressing Ramos cell binding to VCAM coated plates.

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Year:  2001        PMID: 11140722     DOI: 10.1016/s0960-894x(00)00582-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Combinatorial approaches to inhibitors of VLA-4: piperazine-peptoid-bisarylureas.

Authors:  I Lewis; B Rohde; M Mengus; M Weetall; S Maida; R Hugo; P Lake
Journal:  Mol Divers       Date:  2000       Impact factor: 2.943

  1 in total

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