European journal of medicinal chemistry · 2019
Current advances of triazole alcohols derived from fluconazole: Design, in vitro and in silico studies.
СтатьяОбзорНазвание и аннотация: Перевод пока не подготовлен
Обработка статьи · этапы, ошибки и управление
Загрузка состояния…
Ошибки и ограничения
История · было → стало
Состояние обновляется каждые 5 секунд, пока блок открыт. Процент показывается только там, где известен объём работы. Пауза останавливает продолжение этапа; текущий запрос к источнику может завершиться.
Emami Saeed, Ghobadi Elham, Saednia Shahnaz, Hashemi Seyedeh Mahdieh
Аннотация
Currently, the available antifungal agents have significant clinical incompetency in terms of their clinical efficacy, antifungal spectrum, unfavorable pharmacokinetic profiles, substantial side effects and drug-drug interactions. Thus, the optimization and improvement of existing drugs and identification of new antifungal agents are urgently needed. Fluconazole is the first triazole alcohol drug with good in vivo efficacy against yeasts and well-known targets in fungal cells. However, the wide use of fluconazole as a first-line antifungal therapy has led to the development of resistance in clinical isolates of Candida species including Candida albicans and the emerging non-albicans Candida spp. In the last years, extensive efforts inflected to design and discovery of triazole alcohols derived from fluconazole by replacing one triazole ring with the proper side chain. In this paper, we have reviewed the structural modification of fluconazole to pursuit potent triazole alcohols with improved anti-Candida activity, and have highlighted their in vitro activities and in silico studies.