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合成水杨酰苯胺衍生物的抗菌作用及毒性

Antibacterial effect and toxicity of synthesized salicylanilide derivatives.

作者信息

Ghazi I M, Mohamed Z A, Ismail S A, Kamal A

出版信息

Zentralbl Mikrobiol. 1986;141(3):225-32.

PMID:3094282
Abstract

5 nitro- and chloro-salicylanilide derivatives were synthesized by a simple condensation reaction between phenylsalicylate and the required nitroaniline derivative. The compounds were subjected to direct chlorination in CCl4 without any catalyst and were identified by microanalysis, m. p. and spectral studies. The antibacterial activity was investigated against Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, and Staphylococcus aureus. The prepared derivatives were evaluated for their acute toxicity on Swiss albino mice. The compounds 5,2'-dichloro-4'-nitrosalicylanilide and salicyl-3'-nitroanilide were the most active against the test organisms, but they showed fluctuating toxicity effect at the dose of 500 mg/kg. The structure-activity relationship and the toxicity tests verified the compound salicyl-4'-nitroanilide as a reasonable antibacterial agent against the four test organisms without any sign of toxicity symptoms up to the dose of 1000 mg/kg.

摘要

通过水杨酸苯酯与所需的硝基苯胺衍生物之间简单的缩合反应合成了5种硝基和氯代水杨酰苯胺衍生物。这些化合物在四氯化碳中无任何催化剂的情况下进行直接氯化,并通过微量分析、熔点和光谱研究进行鉴定。研究了它们对大肠杆菌、枯草芽孢杆菌、铜绿假单胞菌和金黄色葡萄球菌的抗菌活性。评估了所制备的衍生物对瑞士白化小鼠的急性毒性。化合物5,2'-二氯-4'-亚硝基水杨酰苯胺和水杨酰-3'-硝基苯胺对受试微生物的活性最高,但在500mg/kg剂量下显示出波动的毒性作用。构效关系和毒性试验证实,水杨酰-4'-硝基苯胺是一种对四种受试微生物有效的抗菌剂,在1000mg/kg剂量下无任何毒性症状迹象。

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