Design, synthesis, and antimicrobial evaluation of some nifuroxazide analogs against nosocomial infection,Journal of Heterocyclic Chemistry

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Design, synthesis, and antimicrobial evaluation of some nifuroxazide analogs against nosocomial infection
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-01-21 , DOI: 10.1002/jhet.3891
Deepak K. Dwivedi _{1,

2} , Adarsh Sahu ₁ , Sachin J. Dighade ₂ , Ram Kishore Agrawal ₁

Affiliation

A series of 10 p‐substitutedbenzoylmethylene hydrazide derivatives 4a‐j were synthesized by protecting carboxylic group of 4‐hydroxybenzoic acid using methanol and sulfuric acid than reacting it with hydrazide to form 4‐hydroxybenzohydrazide followed by reacting with a variety of aldehydes and evaluated for their activity against nosocomial infection. All the synthesized compounds were characterized by Fourier‐transform infrared (FT‐IR), ¹H nuclear magnetic resonance (NMR), and mass spectral data. The in vitro antimicrobial potential of synthesized compounds was estimated against prominent strains of nosocomial pathogens (Staphylococcus aureus, Escherichia coli, and Aspergillus niger). The antimicrobial evaluation revealed compounds 4b, 4c, 4d, 4e, 4f, and 4j to be the most active compounds of the series with IC₅₀ value for antibacterial in the range 0.39 to 0.75 μM/mL. Furthermore, the in vitro cytotoxic potential of the compounds was appraised by hemolytic assay. The results showed that some of the synthesized compounds exhibited marked activity.

中文翻译：

设计，合成和某些尼古拉嗪类似物对医院感染的抗菌评估

通过使用甲醇和硫酸保护4-羟基苯甲酸的羧基，然后使其与酰肼反应形成4-羟基苯甲酰肼，然后与多种醛反应，合成了一系列10种对位的苯甲酰基亚甲基酰肼衍生物4a-j。抵抗医院感染的活动。所有合成的化合物均具有傅里叶变换红外（FT-IR），¹ H核磁共振（NMR）和质谱数据的特征。估计合成化合物对医院病原体（金黄色葡萄球菌，大肠埃希菌和黑曲霉）的显着菌株的体外抗菌潜力。）。抗菌评估显示，化合物4b，4c，4d，4e，4f和4j是该系列中活性最高的化合物，抗菌的IC ₅₀值在0.39至0.75μM/ mL范围内。此外，通过溶血测定法评估了化合物的体外细胞毒性潜力。结果表明，某些合成的化合物表现出明显的活性。

更新日期：2020-01-22

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