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0408U004909,
к.фарм.н.
31-10-2008
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Synthesis, structure and biological properties of 1-hydroxy-3-oxo-5,6-dihydro-3H-pyrrolo[3,2,1-ij]quinoline-2-carboxylic acid derivatives
Mospanova Olena Volodymyrivna,
popup.head Ukrayinets' Igor Vasyl'ovych
popup.opponent Петюнін Г.П.
popup.opponent Яременко Ф.Г.
. Як потенційні біологічно активні речовини здійснено синтез великої групи похідних 1-гідрокси-3-оксо-5,6-дигідро-3Н-піроло[3,2,1-i,j]хінолін-2-карбонової кислоти. Для більш ефективного одержання вихідного етилового ефіру 1-гідрокси-3-оксо-5,6-дигідро-3Н-піроло[3,2,1-ij]хінолін-2-карбонової кислоти кон-денсацію індоліну з триетилметантрикарбоксилатом запропоновано проводити при температурі 215 °С і еквімолярному співвідношенні реагентів. Методом дерівато-графії вивчена термічна поведінка проміжних продуктів даної реакції, що дозволило при гетероциклізації уникати утворення небажаного метан-три-N-(індолін-1-іл)-карбоксаміду. Розроблені препаративні методики амідування етилового ефіру 1-гідрокси-3-оксо-5,6-дигідро-3Н-піроло[3,2,1-ij]хінолін-2-карбонової кислоти алкіл-, арилалкіл-, арил- та гетериламінами. Здійснено синтез гідразиду 1-гідрокси-3-оксо-5,6-дигідро-3Н-піроло[3,2,1-ij]хінолін-2-карбонової кислоти. Встановлена нестій-кість цієї сполуки при підвищеній температурі, що необхідно враховувати при її подальших хімічних перетвореннях. Вивчена протитуберкульозна, діуретична і протизапальна активність синтезованих речовин, що дало змогу виявити певні закономірності взаємозв'язку "структурта - дія" та рекомендувати для поглибленого фармакологічного дослідження 4-метоксіанілід 1-гідрокси-3-оксо-5,6-дигідро-3Н-пі-роло[3,2,1-ij]хінолін-2-карбонової кислоти як перспективний діуретик принципово нового хімічного класу
2008-10-31
2020-04-04
Updated: 2025-12-07
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