Анализ перспектив синтеза и применения новых противомикробных субстанций на основе тиетанилированного урацила
Аннотация
Обобщены данные синтеза новых гидразонпроизводных N1-(2-оксопропил)-N3-(1-оксотиетанил, 1,1-диоксотиетанил)-6-метилурацила, и скрининг их противомикробной активности. Оксопропил- и гидразонпроизводные синтезировали по разработанным нами методикам, которые получены на основе реакции алкилирования исходных N3-тиетанилированных модификаций 6-метилурацила с 1,5 кратным избытком 1-хлорпропан-2-она. Реакции осуществляли в среде ацетона или ацетонитрила, в зависимости от степени окисления атома серы, в тиетановом фрагменте. Для синтезированных соединений, предварительно проводили скрининг биологической активности in silico. Кроме того, проведен анализ биологической доступности и проанализирован экономический аспект синтеза в расчёте на один грамм вещества в сравнении с запатентованным препаратом цефтриаксон. Анализ противомикробной активности in vitro, осуществляли по стандартным методикам микробиологических исследований. Выявлены новые соединения, которые проявляют противомикробную активность широкого спектра, показатели минимальной ингибирующей концентрации которой превышают значения для цефтриаксона.
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