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Synthesis, Antibacterial and Anticancer Activity of 1,2-Substituted 2,3-Dihydro-1 H -Benzo[4,5]Imidazo[1,2-c][1,3,2]Diazaphosphol-1-Oxides
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-11-25 , DOI: 10.1007/s11094-020-02282-z
V. Sankar , Vinnie Cheeran , M. R. Ganesh , B. Sivakumar

A series of new 1,2-substituted 2,3-dihydro-1H-benzo[4,5]imidazo[1,2-c][1,3,2]diazaphosphol-1-oxides (5a – 5j) were synthesized and characterized by IR and NMR (1H, 13C, and 31P) spectral analysis. The resulting compounds were studied for their antibacterial and antiproliferative activity. Compounds 5f, 5c and 5g showed significantly higher antibacterial activity against both E. Coli and B. Subtilis compared to other compounds. Similarly, MTT assay using THP-I cells showed that all these compounds had significant antiproliferative activity compared to the solvent control, with compounds 5i, 5g and 5c showing more potency than others. The obtained results suggest that compounds 5a – 5j can have a wide variety of pharmaceutical applications.



中文翻译:

1,2-取代的2,3-二氢-1 H-苯并[4,5]咪唑[1,2-c] [1,3,2]二氮杂膦-1-氧化物的合成,抗菌和抗癌活性

一系列新的1,2-取代的2,3-二氢-1 H-苯并[4,5]咪唑[1,2-c] [1,3,2]二氮杂膦-1-氧化物(5a – 5j)为合成并通过IR和NMR(1 H,13 C和31 P)光谱分析进行表征。研究了所得化合物的抗菌和抗增殖活性。与其他化合物相比,化合物5f,5c5g大肠杆菌枯草芽孢杆菌均显示出明显更高的抗菌活性。同样,使用THP-I细胞的MTT分析表明,与溶剂对照(化合物5i,5g)相比,所有这些化合物均具有显着的抗增殖活性5c则显示出比其他公司更高的效能。获得的结果表明,化合物5a – 5j可以具有广泛的制药应用。

更新日期:2020-11-25
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