<p>An approach to the synthesis of previously unknown ferrocenyl-containing [1,2,4]triazolo[1,5-<i>a</i>]pyrimidin-7-amines was proposed. α-Formylferrocenylacetonitrile was shown to enter the heterocyclization reaction with amino-1,2,4-triazoles to form the target compounds in 50–60% yields. A study of the esterase profile, antioxidant activity in the ABTS (radical-scavenging activity) and FRAP (ferric-reducing antioxidant power) tests, as well as the antiaggregatory activity against β-amyloid (inhibition of AChE-induced and self-aggregation of β-amyloid), of the obtained conjugates showed that the ferrocenyl-containing [1,2,4]triazolo[1,5-<i>a</i>]pyrimidin-7-amines are promising for developing multifunctional drugs for the treatment of Alzheimer’s disease.</p>

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Synthesis and biological activity of 6-ferrocenyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amines

  • P. O. Serebrennikova,
  • Yu. A. Paznikova,
  • E. D. Kazakova,
  • E. A. Kirnos,
  • A. A. Musikhina,
  • E. V. Rudakova,
  • N. V. Kovaleva,
  • N. P. Boltneva,
  • I. N. Ganebnykh,
  • G. F. Makhaeva,
  • I. A. Utepova,
  • O. N. Chupakhin

摘要

An approach to the synthesis of previously unknown ferrocenyl-containing [1,2,4]triazolo[1,5-a]pyrimidin-7-amines was proposed. α-Formylferrocenylacetonitrile was shown to enter the heterocyclization reaction with amino-1,2,4-triazoles to form the target compounds in 50–60% yields. A study of the esterase profile, antioxidant activity in the ABTS (radical-scavenging activity) and FRAP (ferric-reducing antioxidant power) tests, as well as the antiaggregatory activity against β-amyloid (inhibition of AChE-induced and self-aggregation of β-amyloid), of the obtained conjugates showed that the ferrocenyl-containing [1,2,4]triazolo[1,5-a]pyrimidin-7-amines are promising for developing multifunctional drugs for the treatment of Alzheimer’s disease.