Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

Synthesis and Biological Evaluation of 1,2,4-Triazolo[2,3-a]pyrrole Derivatives as Alpha-4 ( α4) Integrin Antagonists

Author(s): Edward C. Lawson, William A. Kinney, Rosemary J. Santulli, Carol M. Fisher, Bruce P. Damiano, Bruce E. Maryanoff.

Abstract:

In exploring for templates to devise novel antagonists for the integrins α4β1 and α4β7, was a series of compounds identified possessing a 1,2,4-triazolo[2,3-a]pyrrole structural subunit. Compound 11, for example, was found to antagonize α4β1-VCAM-1 and α4β7-MAdCAM-1 adhesion with IC50 values of 80 and 20 nM, respectively.

Keywords: Integrin receptors, VCAM-1, arylcarboxamido, pharmacokinetics, LDT-based peptides

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 2
ISSUE: 8
Year: 2005
Page: [601 - 605]
Pages: 5
DOI: 10.2174/157018005774717280
Price: $58