Селективные ингибиторы карбоксилэстеразы для повышения эффективности, безопасности и рационального применения лекарственных препаратов, содержащих сложноэфирные группы

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Опубликован: Jul 12, 2018
DOI: https://doi.org/10.18097/BMCRM00026
Ключевые слова:
карбоксилэстеразы пролекарства лекарства со сложноэфирными группами ингибиторы полифторалкил-2-имино-1,3-дионовый скаффолд

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Н.П. Болтнева
Институт физиологически активных веществ Российской академии наук, 142432 г. Черноголовка Московской обл., Северный проезд, 1
Г.Ф. Махаева
Институт физиологически активных веществ Российской академии наук, 142432 г. Черноголовка Московской обл., Северный проезд, 1
Е.В. Щегольков
Институт органического синтеза им. И.Я. Постовского Уральского отделения РАН, 620990, Екатеринбург, ул. С. Ковалевской, 22/ул. Академическая, 20
Я.В. Бургарт
Институт органического синтеза им. И.Я. Постовского Уральского отделения РАН, 620990, Екатеринбург, ул. С. Ковалевской, 22/ул. Академическая, 20
В.И. Салоутин
Институт органического синтеза им. И.Я. Постовского Уральского отделения РАН, 620990, Екатеринбург, ул. С. Ковалевской, 22/ул. Академическая, 20

Аннотация

В клинической практике применяется большое число пролекарств и активных лекарственных средств, содержащих сложноэфирную, карбаматную или амидную группировку. Ключевым ферментом гидролитического метаболизма таких препаратов в организме являются карбоксилэстеразы (КЭ, КФ 3.1.1.1), которые в значительной степени определяют их фармакокинетику, эффективность и возможные токсические эффекты этих лекарственных средств. Использование селективных ингибиторов КЭ в качестве компонентов комбинированной лекарственной терапии позволяет регулировать скорость гидролитического превращения лекарственных препаратов со сложноэфирной группой и открывает возможность их рационального использования. Создание эффективных и селективных ингибиторов КЭ для применения in vivo, является новым перспективным подходом в медицинской химии и фармакологии, позволяющим повысить эффективность, биодоступность и снизить побочные эффекты многочисленных лекарственных средств, содержащих сложноэфирные группировки.

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Как цитировать
Болтнева N., Махаева G., Щегольков E., Бургарт Y., & Салоутин V. (2018). Селективные ингибиторы карбоксилэстеразы для повышения эффективности, безопасности и рационального применения лекарственных препаратов, содержащих сложноэфирные группы. Biomedical Chemistry: Research and Methods, 1(3), e00026. https://doi.org/10.18097/BMCRM00026
Выпуск
Том 1 № 3 (2018)
Раздел
ОБЗОРЫ

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