Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistantStaphylococcus aureus

Alnufaie Rawan; Alsup Nickolas; Raj K. C. Hansa; Newman Matthew; Whitt Jedidiah; Chambers Steven Andrew; Gilmore David; Alam Mohammad A.

首页> 外文期刊>The Journal of Antibiotics: An International Journal >Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistantStaphylococcus aureus

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Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistantStaphylococcus aureus

机译：4- [4-甲基-3-（2-萘基）吡唑-1-基]苯甲酸衍生物的设计与合成苯甲酸衍生物，其抗药物抗性抑制剂aureus

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We report the synthesis and antimicrobial studies of a new series of naphthyl-substituted pyrazole-derived hydrazones. Many of these novel compounds are potent growth inhibitors of several strains of drug-resistant bacteria. These potent compounds have inclined growth inhibitory properties for planktonicStaphylococcus aureusandAcinetobacter baumannii, and its drug-resistant variants with minimum inhibitory concentration (MIC) as low as 0.78 and 1.56 mu g ml(-1), respectively. These compounds also show potent activity againstS. aureusandA. baumanniibiofilm formation and eradication properties. Time Kill Assay shows that these compounds are bactericidal forS. aureusand bacteriostatic forA. baumannii. The probable mode of action is the disruption of the bacterial cell membrane. Furthermore, potent compounds are nontoxic to human cell lines at several fold higher concentrations than the MICs.

机译：我们报道了一系列新的萘取代吡唑衍生腙的合成和抗菌研究。这些新化合物中有许多是几种耐药细菌的有效生长抑制剂。这些有效化合物对金黄色葡萄球菌和鲍曼菌及其耐药变种具有倾斜生长抑制特性，最低抑制浓度（MIC）分别低至0.78和1.56μg ml（-1）。这些化合物还表现出强大的抗肿瘤活性。奥鲁萨达。鲍曼尼膜的形成和根除特性。杀时试验表明，这些化合物对细菌具有杀菌作用。金黄色和抑菌孔。鲍曼尼。可能的作用方式是破坏细菌细胞膜。此外，强效化合物对人类细胞系无毒，其浓度比MIC高出数倍。

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《The Journal of Antibiotics: An International Journal》 |2020年第12期|共10页
作者
Alnufaie Rawan; Alsup Nickolas; Raj K. C. Hansa; Newman Matthew; Whitt Jedidiah; Chambers Steven Andrew; Gilmore David; Alam Mohammad A.;
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作者单位

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Biol Sci Jonesboro AR 72467 USA;

Arkansas State Univ Coll Sci &

Math Dept Chem &

Phys Jonesboro AR 72467 USA;

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正文语种 eng
中图分类药学;
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Design and synthesis of 4-[4-formyl-3-(2-naphthyl)pyrazol-1-yl]benzoic acid derivatives as potent growth inhibitors of drug-resistantStaphylococcus aureus

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