Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Department of Medical Mycology & Parasitology/Invasive Fungi Research Center (IFRC), Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran.
Future Med Chem. 2018 May 1;10(9):987-1002. doi: 10.4155/fmc-2017-0295. Epub 2018 Apr 23.
A new series of triazole alcohol antifungals 8a-j were designed by introducing benzylthio functionality on one triazole ring of fluconazole.
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.
The prototype compound 8b could be considered as a new lead for design and development of potent antifungal agents. [Formula: see text].
通过在氟康唑的一个三唑环上引入苄硫基官能团，设计了一系列新型三唑醇抗真菌化合物 8a-j。
对目标化合物针对 16 株念珠菌分离株的抗真菌活性评估表明，所有 MIC 值为 0.063-1μg/ml 的化合物与氟康唑（MICs=0.5-4μg/ml）相比，对氟康唑敏感分离株的活性谱更好。特别是代表性化合物 8b 和 8e 对氟康唑耐药的白色念珠菌和近平滑念珠菌分离株也具有活性（MICs=0.063-16μg/ml）。对 Hep-G2 和 NIH-3T3 细胞系的细胞毒性测定表明，这些化合物在非细胞毒性浓度下可显示出很强的抗真菌活性。
原型化合物 8b 可被视为设计和开发强效抗真菌药物的新先导化合物。[化学式：见正文]。
