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探索噻唑骨架以鉴定用于治疗氟康唑耐药念珠菌的新药物。

Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida.

作者信息

Meleddu Rita, Distinto Simona, Corona Angela, Maccioni Elias, Arridu Antonella, Melis Claudia, Bianco Giulia, Matyus Peter, Cottiglia Filippo, Sanna Adriana, De Logu Alessandro

机构信息

a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .

b Department of Organic Chemistry , Semmelweis University Hogyes Endre U , Budapest , Hungary , and.

出版信息

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1672-7. doi: 10.3109/14756366.2015.1113171. Epub 2016 Jan 8.

DOI:10.3109/14756366.2015.1113171
PMID:26745285
Abstract

Cyclohexyliden- and 2-methylcyclohexyliden-hydrazo-4-arylthiazoles were synthesized and tested as antifungal agents. All compounds exhibited minimal inhibitory concentration (MIC) values comparable with those of fluconazole (FLC). Moreover, some compounds showed fungicidal activity at low concentration. Worth noting five out of nine compounds were active towards Candida albicans 25 FLC resistant isolated from clinical specimens. The cellular toxicity was evaluated and none of the compounds is toxic at the MIC. On the basis of our data we can conclude that these derivatives are promising agents for the treatment of resistant C. albicans.

摘要

合成了环己叉基和2-甲基环己叉基肼基-4-芳基噻唑,并将其作为抗真菌剂进行了测试。所有化合物的最低抑菌浓度(MIC)值与氟康唑(FLC)相当。此外,一些化合物在低浓度下表现出杀菌活性。值得注意的是,九种化合物中有五种对从临床标本中分离出的耐氟康唑白色念珠菌25有活性。评估了细胞毒性,在MIC浓度下没有一种化合物有毒。根据我们的数据,我们可以得出结论,这些衍生物是治疗耐药白色念珠菌的有前景的药物。

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