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Eco-Friendly Synthesis, Characterization and Biological Evaluation of Some Novel Pyrazolines Containing Thiazole

Mastoura M Edrees^1,2, Sraa Abu- Melha³, Amirah M Saad⁴

¹Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia. mmohamededrees@yahoo.com.

Molecules (Basel, Switzerland)

|November 17, 2018

Abstract:

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.

Keywords:

anticancer activity antimicrobial activity hydrazonoyl halides pyrazolines thiazoles

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