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

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

Volume: 2 Issue: 8

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

Affiliation:

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

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.

Cite this article as:

Lawson C. Edward, Kinney A. William, Santulli J. Rosemary, Fisher M. Carol, Damiano P. Bruce and Maryanoff E. Bruce, Synthesis and Biological Evaluation of 1,2,4-Triazolo[2,3-a]pyrrole Derivatives as Alpha-4 ( α4) Integrin Antagonists, Letters in Drug Design & Discovery 2005; 2 (8) . https://dx.doi.org/10.2174/157018005774717280