Attempts to Access a Series of Pyrazoles Lead to New Hydrazones with Antifungal Potential against Candida species including Azole-Resistant Strains

被引：0

作者：

Negru, Georgiana ^{[1
]}

Kamus, Laure ^{[2
]}

Bicu, Elena ^{[1
]}

Shova, Sergiu ^{[3
]}

Sendid, Boualem ^{[2
]}

Dubar, Faustine ^{[2
]}

Ghinet, Alina ^{[1
,4
,5
]}

机构：

[1] Alexandru Ioan Cuza Univ, Fac Chem, Bd Carol I 11, Iasi 700506, Romania

[2] Univ Lille, CHU Lille, Inserm U1285,Unite Glycobiol Struct & Fonct, UGSF UMR CNRS 8576,Glycobiol Fungal & Clin Applic, F-59000 Lille, France

[3] Petru Poni Inst Macromol Chem, Iasi 700487, Romania

[4] Hlth & Environm Dept, Lab Sustainable Chem & Hlth, F-59000 Lille, France

[5] Univ Lille, CHU Lille, INSERM,Inst Pasteur Lille, U1167 RID AGE Facteurs Risque & Determinants Mol, F-59000 Lille, France

来源：

MOLECULES | 2021年 / 26卷 / 19期

关键词：

hydrazone; Candida species; antifungal agents; Candida albicans; Candida glabrata; ESCMID-ASTERISK GUIDELINE; MANAGEMENT; DIAGNOSIS;

D O I：

10.3390/molecules26195861

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu g/mL and selective antifungal activity over cytotoxicity.

引用

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