Characterization of antiviral activity of new compounds from the capsid-binding agents group against enteroviruses
Loading...
Date
Journal Title
Journal ISSN
Volume Title
Publisher
Abstract
Энтеровирусы очень распространённые и, к сожалению, опасные патогены. Ситуацию усугубляет то, что против них нет эффективных и универсальных лекарств. Не так давно было открыто новое вещество – 4-(4-(1,3-диоксоизоиндолин-2-ил)фенилсульфонамидо)бензойная кислота. Данное вещество является капсид-связывающим агентом. Мы решили провести первичный скрининг производных данного вещества, а также рассчитать индекс селективности для производных препарата и определить соединения лидеры. В процессе исследований мы идентифицировали два новых соединения с высокой активностью против штамма Коксакивируса B3, которые немного превосходят эталонное соединение. Оба препарата изменили тепловую инактивацию CVB3 in vitro на более высокие температуры, предполагая, что они связывают капсид, как исходное соединение. Полученные результаты могут служить основой для дальнейшей разработки соединений-лидеров для создания новых препаратов для борьбы с энтеровирусной инфекцией.
Enteroviruses are very common and, unfortunately, dangerous pathogens. The situation is aggravated by the fact that there are no effective and universal drugs against them. Not so long ago, a new substance was discovered – 4-(4-(1,3-dioxoisoindolin-2-yl) phenylsulfonamido) benzoic acid. This substance is a capsid-binding agent. We decided to conduct a primary screening of the derivatives of this substance, as well as calculate the selectivity index for the derivatives of the drug and determine the leader compounds. In the course of research, we have identified two new compounds with high activity against the Coxsackievirus B3 strain, which are slightly superior to the reference compound. Both drugs changed the in vitro heat inactivation of CVB3 to higher temperatures, suggesting that they bind the capsid like the parent compound. The results obtained can serve as a basis for further development of leading compounds for the creation of new drugs to combat enterovirus infection.
Enteroviruses are very common and, unfortunately, dangerous pathogens. The situation is aggravated by the fact that there are no effective and universal drugs against them. Not so long ago, a new substance was discovered – 4-(4-(1,3-dioxoisoindolin-2-yl) phenylsulfonamido) benzoic acid. This substance is a capsid-binding agent. We decided to conduct a primary screening of the derivatives of this substance, as well as calculate the selectivity index for the derivatives of the drug and determine the leader compounds. In the course of research, we have identified two new compounds with high activity against the Coxsackievirus B3 strain, which are slightly superior to the reference compound. Both drugs changed the in vitro heat inactivation of CVB3 to higher temperatures, suggesting that they bind the capsid like the parent compound. The results obtained can serve as a basis for further development of leading compounds for the creation of new drugs to combat enterovirus infection.