Microwave-Assisted Syntheses of Amino Acid Ester Substituted Benzoic Acid Amides: Potential Inhibitors of Human CD81-Receptor HCV-E2 Interaction

Marcel Holzer; Sigrid Ziegler; Bernd Kronenberger; Christian D Klein; Rolf W Hartmann

doi:10.2174/1874104500802010021

Microwave-Assisted Syntheses of Amino Acid Ester Substituted Benzoic Acid Amides: Potential Inhibitors of Human CD81-Receptor HCV-E2 Interaction

Open Med Chem J. 2008 Apr 15:2:21-5. doi: 10.2174/1874104500802010021.

Authors

Marcel Holzer¹, Sigrid Ziegler, Bernd Kronenberger, Christian D Klein, Rolf W Hartmann

Affiliation

¹ Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D-66041 Saarbrücken, Germany.

Abstract

Results from our group showed benzyl salicylate to be a moderate inhibitor of the CD81-LEL-HCV-E2 interaction. To increase the biological activity, heterocyclic substituted benzoic acids were coupled to amino acid esters via microwave assisted DCC-reaction. The prepared compounds were tested for their inhibitory potency by means of a fluorescence labeled antibody assay system using HUH7.5 cells.

Keywords: CD81-receptor; Hepatitis C virus; benzyl salicylate; large extracellular loop; microwave assisted amide syntheses; protein-protein interaction..