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<p>Eight ethyl 4-aryl-2-oxo-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-<i>a</i>]pyrimidine-3-carboxylates were resynthesized. Ideas about their spatial structures were expanded. Acute toxicity was assessed using the V. B. Prozorovsky express method; the analgesic effect, using the acetic-acid writhing test of the synthesized compounds. Five compounds with low acute toxicity, the analgesic activity of which exceeded the effect of metamizole sodium, were identified. The number of acetic writhings decreased by more than 70% under their influence in experimental animals. It was established that this class of compounds is promising for further discovery of biologically active compounds with analgesic activity.</p>

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Study of Structural Features and Assessment of Acute Toxicity and Analgesic Effects of Ethyl 4-Aryl-2-Oxo-1,2,3,4-Tetrahydrobenzo[4,5]Imidazo-[1,2-a]Pyrimidine-3-Carboxylates

  • 期刊论文

  • 发表日期：

    2025年9月1日

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  • K. V. Podchezertseva,
  • N. A. Buzmakova,
  • T. M. Zamaraeva,
  • I. P. Rudakova,
  • M. V. Dmitriev

摘要

Eight ethyl 4-aryl-2-oxo-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrimidine-3-carboxylates were resynthesized. Ideas about their spatial structures were expanded. Acute toxicity was assessed using the V. B. Prozorovsky express method; the analgesic effect, using the acetic-acid writhing test of the synthesized compounds. Five compounds with low acute toxicity, the analgesic activity of which exceeded the effect of metamizole sodium, were identified. The number of acetic writhings decreased by more than 70% under their influence in experimental animals. It was established that this class of compounds is promising for further discovery of biologically active compounds with analgesic activity.