<p>A series of new ferrocene conjugates containing 1<i>H</i>-1,2,3-triazole moieties was prepared by the Cu-catalyzed azide-alkyne cycloaddition. The new compounds were evaluated as potential drugs for the treatment of concomitant multifactorial diseases, such as Alzheimer’s disease and type 2 diabetes mellitus. The study included the analysis of the esterase profile, the assessment of the ability to inhibit the β-amyloid (1–42) self-aggregation, and the evaluation of the primary antioxidant activity of the new compounds. The synthesized conjugates showed a high radical scavenging capacity in the ABTS assay and the ferric reducing capacity in the FRAP assay, exhibited high inhibitory activity against the β-amyloid (1–42) self-aggregation, and displayed moderate inhibition of butyrylcholinesterase.</p>

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Ferrocene-containing 1,4-disubstituted 1H-1,2,3-triazoles with high antioxidant and anti-aggregation activity

  • T. S. Skornyakova,
  • G. F. Makhaeva,
  • E. Yu. Zyryanova,
  • A. A. Musikhina,
  • E. V. Rudakova,
  • N. V. Kovaleva,
  • N. P. Boltneva,
  • P. O. Konarev,
  • M. A. Kiskin,
  • I. A. Utepova,
  • O. N. Chupakhin

摘要

A series of new ferrocene conjugates containing 1H-1,2,3-triazole moieties was prepared by the Cu-catalyzed azide-alkyne cycloaddition. The new compounds were evaluated as potential drugs for the treatment of concomitant multifactorial diseases, such as Alzheimer’s disease and type 2 diabetes mellitus. The study included the analysis of the esterase profile, the assessment of the ability to inhibit the β-amyloid (1–42) self-aggregation, and the evaluation of the primary antioxidant activity of the new compounds. The synthesized conjugates showed a high radical scavenging capacity in the ABTS assay and the ferric reducing capacity in the FRAP assay, exhibited high inhibitory activity against the β-amyloid (1–42) self-aggregation, and displayed moderate inhibition of butyrylcholinesterase.