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新型有机砷化合物的微量热法抗菌评价。

Antibacterial evaluation of novel organoarsenic compounds by the microcalorimetric method.

机构信息

State Key Laboratory of Virology, College of Chemistry and Molecule Sciences, Wuhan University, 430072 Wuhan, People's Republic of China.

出版信息

Biol Trace Elem Res. 2013 Jun;153(1-3):382-9. doi: 10.1007/s12011-013-9660-5. Epub 2013 Apr 20.

Abstract

Antibacterial activities of novel organoarsenic compounds As(III)-containing Schiff bases on Escherichia coli (CCTCCAB91112) were investigated by microcalorimetry in this study. The experimental result showed that the arsenic(III)-containing Schiff bases at micromolar concentration exhibit strong inhibition on the E. coli. Specifically, the growth rate constant k decreased, and the generation time t G and the inhibitory ratio I (percentage) increased with the increased dose of the arsenicals as inhibitors. All of the arsenicals display the feature of considerable lag phase inhibition on the cell growth. The compound 4-(4-bromobenzaliminyl)phenylarsenoxide makes the lag phase of E. coli cell growth cycles to reach 650 min at 5 μmol/L. The compounds with donating electron groups at aromatic ring B have lower IC50 to present higher antibacterial activity. The compound 4-(4-hydroxyl-3-methoxylbenzaliminyl)phenylarsenoxide has the lowest IC50 (1.82 μmol/L) to show the strongest antibacterial activity among them.

摘要

本研究采用微量热法研究了新型含砷有机化合物 Schiff 碱对大肠杆菌(CCTCCAB91112)的抗菌活性。实验结果表明,含砷的 Schiff 碱在微摩尔浓度下对大肠杆菌表现出很强的抑制作用。具体来说,随着砷剂剂量的增加,生长速率常数 k 减小,代时 tG 和抑制率 I(百分比)增加。所有的砷剂都表现出对细胞生长有相当长的迟滞期抑制的特点。化合物 4-(4-溴苯亚氨基)苯胂氧化物使大肠杆菌细胞生长周期的迟滞期在 5 μmol/L 时达到 650 min。苯环 B 上有供电子基团的化合物具有较低的 IC50,表现出更高的抗菌活性。其中,化合物 4-(4-羟基-3-甲氧基苯亚氨基)苯胂氧化物的 IC50 最低(1.82 μmol/L),表现出最强的抗菌活性。

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