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Eco-Friendly Synthesis Characterization and Biological Evaluation of Some Novel Pyrazolines Containing Thiazole Moiety as Potential Anticancer and Antimicrobial Agents

机译:某些新型含噻唑基吡唑啉类化合物作为潜在的抗癌和抗菌剂的生态友好合成表征和生物学评价

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摘要

The one-pot synthesis of a series of pyrazoline derivatives containing the bioactive thiazole ring has been performed through a 1,3-dipolar cycloaddition reaction of N-thiocarbamoylpyrazoline and different hydrazonoyl halides or α-haloketones in the presence of DABCO (1,4-diazabicyclo[2.2.2] octane) as an eco-friendly catalyst using the solvent-drop grinding method. The structure of the synthesized compounds was elucidated using elemental and spectroscopic analyses (IR, NMR, and Mass). The activity of these compounds against human hepatocellular carcinoma cell line (HepG2) was tested and the results showed that the pyrazoline >11f, which has a fluorine substituent, is the most active. The antimicrobial activities of the newly synthesized compounds were determined against two fungi and four bacterial strains, and the results indicated that some of the newly synthesized pyrazolines are more potent than the standard drugs against test organisms.
机译:在DABCO存在下,通过N-硫代氨基甲酰基吡唑啉与不同的酰卤化物或α-卤代酮的1,3-偶极环加成反应进行了一系列包含生物活性噻唑环的吡唑啉衍生物的一锅合成(1,4-二氮杂双环[2.2.2]辛烷)作为一种环保型催化剂,采用溶剂滴磨法。使用元素分析和光谱分析(IR,NMR和质谱)阐明了合成化合物的结构。测试了这些化合物对人肝癌细胞系(HepG2)的活性,结果表明,具有氟取代基的吡唑啉> 11f 具有最高的活性。测定了新合成的化合物对两种真菌和四种细菌菌株的抗菌活性,结果表明,一些新合成的吡唑啉比标准药物对测试生物的效力更高。

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