RESEARCH ARTICLE


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



Marcel Holzer, Sigrid Ziegler, Bernd Kronenberger, Christian D Klein , Rolf W Hartmann;*
Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D-66041 Saarbrücken, Germany


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Creative Commons License
© Holzer et al.; Licensee Bentham Open

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.5/), which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited.

* Address correspondence to this author at the Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 151150, D-66041 Saarbrücken, Germany; Tel: +49 681 302-2424; Fax: +49 681 302-4386; E-mail: rwh@mx.uni-saarland.de


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