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<p>Five compounds of the ethyl 6′-amino-2-oxo-5′-cyano-2′<i>H</i>-spiro[indoline-3,4′-pyrano[2,3-<i>c</i>]pyrazole]-3′-carboxylate series were resynthesized. Acute toxicity was assessed using the express method of V. B. Prozorovsky. Analgesic action of the synthesized compounds was assessed using the acetic writhing technique. It was found that the studied compounds of the spiro[indoline-3,4′-pyrano[2,3-<i>c</i>]pyrazole] series did not have acute toxicity at the studied doses, exhibited analgesic activity, and decreased the number of acetic writhings by 69-91% in experimental animals, exceeding the effect of the reference drug metamizole sodium. The ability of compounds <b>I</b>, <b>II</b>, <b>IV</b>, and <b>V</b>, which were designed based on x-ray diffraction data for compound <b>III</b>, to inhibit cyclooxygenases (COX) 1 and 2 was studied. The highest binding energies to COX1 were found for compound <b>III</b> (–5.29 kcal/mol); to COX2, for compounds <b>I</b> and <b>III</b> (–6.44 and –6.35 kcal/mol, respectively).</p>

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Evaluation of Acute Toxicity and Analgesic Effect of Ethyl 6′-amino-2-oxo-5′-cyano-2′H-spiro[indoline-3,4′-pyrano[2,3-c]pyrazole]-3′-carboxylates

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • A. S. Goman,
  • N. A. Buzmakova,
  • T. M. Zamaraeva,
  • K. V. Andryukov

摘要

Five compounds of the ethyl 6′-amino-2-oxo-5′-cyano-2′H-spiro[indoline-3,4′-pyrano[2,3-c]pyrazole]-3′-carboxylate series were resynthesized. Acute toxicity was assessed using the express method of V. B. Prozorovsky. Analgesic action of the synthesized compounds was assessed using the acetic writhing technique. It was found that the studied compounds of the spiro[indoline-3,4′-pyrano[2,3-c]pyrazole] series did not have acute toxicity at the studied doses, exhibited analgesic activity, and decreased the number of acetic writhings by 69-91% in experimental animals, exceeding the effect of the reference drug metamizole sodium. The ability of compounds I, II, IV, and V, which were designed based on x-ray diffraction data for compound III, to inhibit cyclooxygenases (COX) 1 and 2 was studied. The highest binding energies to COX1 were found for compound III (–5.29 kcal/mol); to COX2, for compounds I and III (–6.44 and –6.35 kcal/mol, respectively).