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Syntheses of Novel 4-Substituted N-(5-amino-1H-124-triazol-3-yl)pyridine-3-sulfonamide Derivatives with Potential Antifungal Activity

机译:具有潜在抗真菌活性的新型4-取代的N-(5-氨基-1H-124-三唑-3-基)吡啶-3-磺酰胺衍生物的合成

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摘要

Candidiasis represent a serious threat for patients with altered immune responses. Therefore, we have undertaken the synthesis of compounds comprising a pyridine-3-sulfonamide scaffold and known antifungally active 1,2,4-triazole substituents. Thus a series of novel 4-substituted N-(5-amino-1H-1,2,4-triazol-3-yl)pyridine-3-sulfonamides have been synthesized by multistep reactions starting from 4-chloropyridine-3-sulfonamide via N′-cyano-N-[(4-substitutedpyridin-3-yl)sulfonyl]carbamimidothioates which were further converted with hydrazine hydrate to the corresponding 1,2,4-triazole derivatives >26–>36. The final compounds were evaluated for antifungal activity against strains of the genera Candida, Geotrichum, Rhodotorula, and Saccharomycess isolated from patients with mycosis. Many of them show greater efficacy than fluconazole, mostly towards Candida albicans and Rhodotorula mucilaginosa species, with MIC values ≤ 25 µg/mL. A docking study of the most active compounds >26, >34 and >35 was performed showing the potential mode of binding to Candida albicans lanosterol 14α-demethylase. Also in vitro cytotoxicity of selected compounds have been evaluated on the NCI-60 cell line panel.
机译:念珠菌病对免疫反应改变的患者构成严重威胁。因此,我们已经进行了包含吡啶-3-磺酰胺支架和已知的抗真菌活性的1,2,4-三唑取代基的化合物的合成。因此,通过从4-氯吡啶-3-磺酰胺开始的多步反应,通过以下步骤合成了一系列新颖的4-取代的N-(5-氨基-1H-1,2,4-三唑-3-基)吡啶-3-磺酰胺。 N'-氰基-N-[(4-取代的吡啶-3-基)磺酰基]氨基甲硫代氨基甲酸酯,再与水合肼转化为相应的1,2,4-三唑衍生物> 26 – > 36 。评估了最终化合物对分离自真菌病患者的念珠菌,大脚草属,杜鹃花属和糖酵母属菌株的抗真菌活性。它们中的许多药物显示出比氟康唑更大的功效,主要针对白色念珠菌和粘菌红假单胞菌,MIC值≤25 µg / mL。对最具活性的化合物> 26 ,> 34 和> 35 进行的对接研究显示了与白色念珠菌羊毛甾醇羊毛甾醇14α-脱甲基酶结合的潜在模式。 NCI-60细胞系还评估了所选化合物的体外细胞毒性。

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