Synthesis and Biological Evaluation of 1,2,4-Triazolo[2,3-a]pyrrole Derivatives as Alpha-4 ( α4) Integrin Antagonists
Edward C. Lawson,
William A. Kinney,
Rosemary J. Santulli,
Carol M. Fisher,
Bruce P. Damiano,
Bruce E. Maryanoff.
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
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