Future medicinal chemistry · 2018
Discovery of benzylthio analogs of fluconazole as potent antifungal agents.
СтатьяПоддержка исследования: вне правительства СШАНазвание 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.
Motahari Kamran, Badali Hamid, Hashemi Seyedeh Mahdieh, Fakhim Hamed, Mirzaei Hassan, Vaezi Afsane, Shokrzadeh Mohammad, Emami Saeed
Аннотация
AIM: A new series of triazole alcohol antifungals 8a-j were designed by introducing benzylthio functionality on one triazole ring of fluconazole.
RESULTS: The antifungal activity evaluation of target compounds against 16 Candida isolates indicated that all compounds with MIC values of 0.063-1 μg/ml had better profile of activity in respect to fluconazole (MICs = 0.5-4 μg/ml) against fluconazole-susceptible isolates. In particular, the representative compounds 8b and 8e were also active against fluconazole-resistant isolates of Candida albicans and Candida parapsilosis (MICs = 0.063-16 μg/ml). Cytotoxicity assay against Hep-G2 and NIH-3T3 cell lines revealed that these compounds can display potent antifungal activity at noncytotoxic concentrations.
CONCLUSION: The prototype compound 8b could be considered as a new lead for design and development of potent antifungal agents. [Formula: see text].
RESULTS: The antifungal activity evaluation of target compounds against 16 Candida isolates indicated that all compounds with MIC values of 0.063-1 μg/ml had better profile of activity in respect to fluconazole (MICs = 0.5-4 μg/ml) against fluconazole-susceptible isolates. In particular, the representative compounds 8b and 8e were also active against fluconazole-resistant isolates of Candida albicans and Candida parapsilosis (MICs = 0.063-16 μg/ml). Cytotoxicity assay against Hep-G2 and NIH-3T3 cell lines revealed that these compounds can display potent antifungal activity at noncytotoxic concentrations.
CONCLUSION: The prototype compound 8b could be considered as a new lead for design and development of potent antifungal agents. [Formula: see text].