Biopolym. Cell. 2021; 37(1):33-45.
Биоорганическая химия
Синтез и диуретическая активность новых производных 5-амино-1,3,4-тиадиазол-2-тиола
1Драпак И. В., 1Зименковский Б. С., 1Слабый М. В., 1, 2Голота С. Н., 3Перехода Л. А., 1Яремкевыч Р. В., 1Нектегаев И. А.
  1. Львовький национальный медицинский университет имени Даниила Галицкого
    ул. Пекарьска, 69, Львов, Украина, 79010
  2. Волынский национальный университет им. Леси Украинки
    пр. Воли, 13, Луцк, Украина, 43025
  3. Национальный фармацевтический университет
    ул. Пушкинская, 53, Харьков, Украина, 61002

Abstract

Цель. Синтез, in vivo исследование и характеристика диуретической активности новых производных 5-амино-1,3,4-тиадиазол-2-тиола. Методы. Органический синтез (однореакторные реакции). 1Н ЯМР-спектроскопия. Биологические методы: in vivo исследование на белых крысах; общий анализ мочи; индексы салуретической, натрийуретической активности и ингибирования карбоангидразы; биохимические лабораторные исследования (определение уровней АЛТ, АСТ, ЩФ, γ-ГГТ, общего билирубина и белка). Результаты. Синтезирована серия производных 5-амино-1,3,4-тиадиазол-2-тиола с использованием эффективного однореакторного подхода. Все соединения исследовались на предмет диуретической активности путем оценки общего суточного диуреза и профиля общего анализа мочи. Идентифицированы 5-бензилтио-1,3,4-тиадиазол-2-амины 2а, 2с и 2е как потенциальные диуретики для которых были исследованы при калийуретические, салуретические и натрийуретические свойства, а также было оценена их способность ингибировать карбоангидразу. Сформулировано завсисимости структура – диуретическое действие. Выводы. Синтезирована серия производных 1,3,4-тиадиазола, среди которой идентифицированы соединения с высоким уровнем диуретического действия и удовлетворительными калиуретическими, салуретическими и натрийуретическими свойствами.
Keywords: производные 5-амино-1,3,4-тиадиазол-2-тиола, диуретическая активность, салуретиче-ская/натрийуретическая активность, ингибирование карбоангидразы, зависимость структура-активность

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