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首页> 美国卫生研究院文献>Pharmaceuticals >In Vitro Assessment of Antimicrobial Antioxidant and Cytotoxic Properties of Saccharin–Tetrazolyl and –Thiadiazolyl Derivatives: The Simple Dependence of the pH Value on Antimicrobial Activity
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In Vitro Assessment of Antimicrobial Antioxidant and Cytotoxic Properties of Saccharin–Tetrazolyl and –Thiadiazolyl Derivatives: The Simple Dependence of the pH Value on Antimicrobial Activity

机译：糖精-四唑基和-噻二唑基衍生物的抗菌抗氧化和细胞毒性特性的体外评估：pH值对抗菌活性的简单依赖

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The antimicrobial, antioxidant, and cytotoxic activities of a series of saccharin–tetrazolyl and –thiadiazolyl analogs were examined. The assessment of the antimicrobial properties of the referred-to molecules was completed through an evaluation of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values against Gram-positive and Gram-negative bacteria and yeasts. Scrutiny of the MIC and MBC values of the compounds at pH 4.0, 7.0, and 9.0 against four Gram-positive strains revealed high values for both the MIC and MBC at pH 4.0 (ranging from 0.98 to 125 µg/mL) and moderate values at pH 7.0 and 9.0, exposing strong antimicrobial activities in an acidic medium. An antioxidant activity analysis of the molecules was performed by using the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, which showed high activity for the TSMT ( -(1-methyl-2 -tetrazol-5-yl)- -(1,1-dioxo-1,2-benzisothiazol-3-yl) amine, ) derivative (90.29% compared to a butylated hydroxytoluene positive control of 61.96%). Besides, the general toxicity of the saccharin analogs was evaluated in an model, which displayed insignificant toxicity values. In turn, upon an assessment of cell viability, all of the compounds were found to be nontoxic in range concentrations of 0–100 µg/mL in H7PX glioma cells. The tested molecules have inspiring antimicrobial and antioxidant properties that represent potential core structures in the design of new drugs for the treatment of infectious diseases.
机译：研究了一系列糖精-四唑基和-噻二唑基类似物的抗微生物，抗氧化剂和细胞毒性活性。通过评估针对革兰氏阳性和革兰氏阴性细菌和酵母菌的最小抑菌浓度（MIC）和最小杀菌浓度（MBC）值，完成了对上述分子的抗菌性能的评估。仔细检查化合物在pH 4.0、7.0和9.0下针对四种革兰氏阳性菌株的MIC和MBC值，发现MIC和MBC在pH 4.0时均具有高值（范围为0.98至125 µg / mL），在pH为4.0时处于中等值pH 7.0和9.0，在酸性介质中具有很强的抗菌活性。通过使用DPPH（2,2-二苯基-1-picylhydrazyl）方法进行分子的抗氧化活性分析，该方法对TSMT（-（1-甲基-2-4-四唑-5-基）-- （1,1-二氧代-1,2-苯并噻唑-3-基）胺衍生物）（90.29％，而丁基化羟基甲苯阳性对照为61.96％）。此外，糖精类似物的一般毒性在模型中进行了评估，显示出微不足道的毒性值。反过来，在评估细胞活力后，发现所有化合物在H7PX胶质瘤细胞中的浓度范围为0–100 µg / mL都是无毒的。被测试的分子具有令人鼓舞的抗微生物和抗氧化特性，这些特性代表了在设计用于治疗传染病的新药物中潜在的核心结构。

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