<p>A selective one-step method for preparing conjugates of glycyrrhizic acid (GA) with amino acids and dipeptides (L-Val, D-Val, L-Leu, D-Leu, L-Phe, D-Phe, Gly-Val, Gly-Leu, Gly-Phe) in 60–65% yields using 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline was proposed. The conjugate of GA with valine exhibited pronounced antiulcer activity in a rat indomethacin gastric ulcer model at a dose of 50 mg/kg.</p>

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Synthesis of Pharmacologically Significant Conjugates of Glycyrrhizic Acid with Amino Acids and Dipeptides Using 2-Ethoxy-1-Ethoxycarbonyl-1,2-Dihydroquinoline

  • A. I. Fairushina,
  • S. F. Petrova,
  • N. S. Makara,
  • T. A. Sapozhnikova,
  • L. A. Baltina

摘要

A selective one-step method for preparing conjugates of glycyrrhizic acid (GA) with amino acids and dipeptides (L-Val, D-Val, L-Leu, D-Leu, L-Phe, D-Phe, Gly-Val, Gly-Leu, Gly-Phe) in 60–65% yields using 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline was proposed. The conjugate of GA with valine exhibited pronounced antiulcer activity in a rat indomethacin gastric ulcer model at a dose of 50 mg/kg.