<p>The mnestic activity of synthetic derivatives of the alkaloid (–)-cytisine with a thiourea substituent in the 3- and 9-position was studied in a conditioned passive avoidance response (CPAR) test. Four candidate compounds with mnestic activity comparable to or exceeding that of the reference drug piracetam were identified among 26 tested derivatives. One of the compounds, the ethyl ester of 2{3-[(1<i>R</i>,5<i>S</i>)-3-methyl-8-oxo-2,3,4,5,6,8-hexahydro-1<i>H</i>-1,5-methanopyrido[1,2-<i>a</i>][1,5]diazocin-9-yl]thioureido}acetic acid, which was prepared by reacting methylcytisine 9-isothiocyanate with ethyl glycinate, exhibited 100% mnestic activity.</p>

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Thioureas of the (–)-Cytisine Series with Mnestic Activity

  • A. V. Koval’skaya,
  • V. A. Sorokina,
  • S. F. Gabdrakhmanova,
  • N. S. Makara,
  • T. A. Sapozhnikova,
  • I. P. Tsypysheva

摘要

The mnestic activity of synthetic derivatives of the alkaloid (–)-cytisine with a thiourea substituent in the 3- and 9-position was studied in a conditioned passive avoidance response (CPAR) test. Four candidate compounds with mnestic activity comparable to or exceeding that of the reference drug piracetam were identified among 26 tested derivatives. One of the compounds, the ethyl ester of 2{3-[(1R,5S)-3-methyl-8-oxo-2,3,4,5,6,8-hexahydro-1H-1,5-methanopyrido[1,2-a][1,5]diazocin-9-yl]thioureido}acetic acid, which was prepared by reacting methylcytisine 9-isothiocyanate with ethyl glycinate, exhibited 100% mnestic activity.