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<p>A series of calcium salts of <i>N</i>-sulfoalkylated lactams with different ring sizes were synthesized. The structures of the new compounds were confirmed by IR and NMR spectroscopy, elemental analysis, and X-ray diffraction analysis. The cytotoxicity of several compounds was evaluated using the MTT assay on the A549, MCF7, NKE, and Raw 264.7 cell lines. Calcium 3-(2-oxopyridin-1-yl)propane-1-sulfonate (<b>11a</b>), calcium 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate (<b>11b</b>), and calcium 3-(2-oxoazepan-1-yl)-propane-1-sulfonate (<b>11d</b>) did not exhibit toxic activity at the maximum concentrations on the Raw 264.7 cell line; compound <b>11a</b> also did not show activity on the NKE cell line. The other salts exhibited moderate toxicity. Based on these data, the selected lead compounds (<b>11a,b,d</b>) were used to evaluate the anti-inflammatory activity. In a lipopolysaccharide-induced inflammatory model, compound <b>11d</b> demonstrated a significant decrease in the expression of IL-1β and COX-2, indicating a pronounced anti-inflammatory activity.</p>

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N-Sulfoalkylated lactams: synthesis, structures, and biological activity

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • M. A. Rudakova,
  • E. P. Kramarova,
  • D. V. Tarasenko,
  • A. A. Korlyukov,
  • A. D. Shagina,
  • A. A. Lagunin,
  • N. Yu. Karpechenko,
  • D. I. Gonchar,
  • Yu. I. Baukov,
  • T. A. Shmigol,
  • Vad. V. Negrebetsky

摘要

A series of calcium salts of N-sulfoalkylated lactams with different ring sizes were synthesized. The structures of the new compounds were confirmed by IR and NMR spectroscopy, elemental analysis, and X-ray diffraction analysis. The cytotoxicity of several compounds was evaluated using the MTT assay on the A549, MCF7, NKE, and Raw 264.7 cell lines. Calcium 3-(2-oxopyridin-1-yl)propane-1-sulfonate (11a), calcium 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate (11b), and calcium 3-(2-oxoazepan-1-yl)-propane-1-sulfonate (11d) did not exhibit toxic activity at the maximum concentrations on the Raw 264.7 cell line; compound 11a also did not show activity on the NKE cell line. The other salts exhibited moderate toxicity. Based on these data, the selected lead compounds (11a,b,d) were used to evaluate the anti-inflammatory activity. In a lipopolysaccharide-induced inflammatory model, compound 11d demonstrated a significant decrease in the expression of IL-1β and COX-2, indicating a pronounced anti-inflammatory activity.