<p>The analgesic activity and acute toxicity of substituted 2-oxocyclohexane-1-carboxamides and 2-oxocyclohex-3-ene-1-carboxamides were studied. It was established that the substituted 4-hydroxy-2-oxocyclohexane-1-carboxamides <b>3a</b>-<b>b</b>, their dehydration products <b>4a</b>-<b>d</b>, and intermediate 1,5-diketone <b>5</b> were low-toxic and practically non-toxic compounds. Compounds <b>3b</b>, <b>4a</b>, <b>4b</b>, <b>4d</b>, and diketone <b>5</b> exhibited antinociceptive activity in the hot-plate test. The most pronounced effect was found for compound <b>5</b>. All studied 4-hydroxy-2-oxocyclohexane-1-carboxamides and their dehydration products, except for <b>4c</b>, reduced the number of contractions of abdominal muscles caused by intraperitoneal administration of acetic acid. The results created the prerequisites for further studies of the mechanisms of analgesic activity of the studied compounds.</p>

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Analgesic Activity of Substituted 4-Hydroxy-2-Oxocyclohexane-1-Carboxamides and Their Dehydration Products

  • O. N. Gein,
  • N. V. Nosova,
  • A. A. Sokolov,
  • E. E. Mavrina,
  • V. L. Gein

摘要

The analgesic activity and acute toxicity of substituted 2-oxocyclohexane-1-carboxamides and 2-oxocyclohex-3-ene-1-carboxamides were studied. It was established that the substituted 4-hydroxy-2-oxocyclohexane-1-carboxamides 3a-b, their dehydration products 4a-d, and intermediate 1,5-diketone 5 were low-toxic and practically non-toxic compounds. Compounds 3b, 4a, 4b, 4d, and diketone 5 exhibited antinociceptive activity in the hot-plate test. The most pronounced effect was found for compound 5. All studied 4-hydroxy-2-oxocyclohexane-1-carboxamides and their dehydration products, except for 4c, reduced the number of contractions of abdominal muscles caused by intraperitoneal administration of acetic acid. The results created the prerequisites for further studies of the mechanisms of analgesic activity of the studied compounds.