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Attempts to Access a Series of Pyrazoles Lead to New Hydrazones with Antifungal Potential against Candida Species Including Azole-Resistant Strains
Molecules ( IF 4.6 ) Pub Date : 2021-09-27 , DOI: 10.3390/molecules26195861
Georgiana Negru 1 , Laure Kamus 2 , Elena Bîcu 1 , Sergiu Shova 3 , Boualem Sendid 2 , Faustine Dubar 2 , Alina Ghinet 1, 4, 5
Affiliation  

The treatment of benzylidenemalononitriles with phenylhydrazines in refluxing ethanol did not provide pyrazole derivatives, but instead furnished hydrazones. The structure of hydrazones was secured by X-ray analysis. The chemical proof was also obtained by direct reaction of 3,4,5-trimethoxybenzaldehyde with 2,4-dichlorophenylhydrazine. Newly synthesized hydrazones were tested against eight Candida spp. strains in a dose response assay to determine the minimum inhibitory concentration (MIC99). Five compounds were identified as promising antifungal agents against Candida spp. (C. albicans SC5314, C. glabrata, C. tropicalis, C. parapsilosis and C. glabrata (R azoles)), with MIC99 values ranging from 16 to 32 µg/mL and selective antifungal activity over cytotoxicity.

中文翻译:

尝试获得一系列吡唑导致具有抗真菌潜力的新型腙对抗念珠菌属物种,包括抗唑菌株

在回流乙醇中用苯肼处理亚苄基丙二腈没有提供吡唑衍生物,而是提供腙。通过X射线分析确定腙的结构。化学证明也通过 3,4,5-三甲氧基苯甲醛与 2,4-二氯苯肼的直接反应获得。新合成的腙针对八种念珠菌进行了测试。剂量反应试验中的菌株以确定最小抑制浓度 (MIC 99 )。五种化合物被鉴定为有前景的抗念珠菌抗真菌剂。(白色念珠菌SC5314,光滑念珠菌热带念珠菌近平滑念珠菌光滑念珠菌( ř唑类),MIC 99值范围从 16 到 32 µg/mL,选择性抗真菌活性超过细胞毒性。
更新日期:2021-09-27
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