Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia.
Department of Organic Chemistry, National Organization for Drug Control and Research (NODAR), Giza 12311, Egypt.
Molecules. 2018 Nov 14;23(11):2970. doi: 10.3390/molecules23112970.
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 -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 , 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.
通过 - 硫代甲酰基吡唑啉与不同的腙卤代物或α-卤代酮在 1,4-二氮杂二环[2.2.2]辛烷（DABCO）作为环保催化剂的存在下的 1,3-偶极环加成反应，一锅法合成了一系列含有生物活性噻唑环的吡唑啉衍生物。使用溶剂滴磨法，通过元素分析和光谱分析（IR、NMR 和 Mass）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是最活跃的。新合成化合物的抗菌活性针对两种真菌和四种细菌菌株进行了测定，结果表明，一些新合成的吡唑啉类化合物对测试生物的活性比标准药物更强。
