Effective synthesis of some novel pyrazolidine-3,5-dione derivatives via Mg(II) catalyzed in water medium and their anticancer and antimicrobial activities
- 23 Downloads
Novel pyrazolidine-3,5-dione derivatives (2a–g, 4a–g, and 6a–g) were synthesized by an easy-to-perform Mg(II) acetylacetonate-catalyzed reaction with high yields using water as the reaction medium. Synthesized compounds were screened for anticancer and antimicrobial activities. The compound 6c (LD50 19.1 µg/mL) showed anticancer activity higher than that of all other compounds against MCF-7 breast cancer cell line. Results of antimicrobial activities revealed that the compound 4d (MIC 0.5 μg/mL) had higher activity than ciprofloxacin against Staphylococcus aureus, whereas the compound 2b (MIC 0.5 μg/mL) had higher activity than clotrimazole against Candida albicans. Overall results of this study envisaged that the compounds 2b, 4d, and 6c have the potential to be developed as anticancer and antimicrobial agents.
KeywordsPyrazolidine-3,5-dione derivative Mg(II) catalysis Antibacterial activity Antifungal activity Anticancer activity
The project was supported by King Saud University, Deanship of Scientific Research, College of Science Research Center.
- 9.Deng G, Li W, Shen J, Jiang H, Chen K, Liu H (2008) Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation. Bioorg Med Chem Lett 18:5497–5502. https://doi.org/10.1016/j.bmcl.2008.09.027 CrossRefPubMedGoogle Scholar
- 10.Gilbert AM, Failli A, Shumsky J, Yang Y, Severin A, Singh G, Hu W, Keeney D, Petersen PJ, Katz AH (2006) Pyrazolidine-3,5-diones and 5-hydroxy-1H-pyrazol- 3(2H)-ones, inhibitors of UDP-N-acetylenolpyruvyl glucosamine reductase. J Med Chem 49:6027–6036. https://doi.org/10.1021/jm060499t CrossRefPubMedGoogle Scholar
- 20.Gillespie SH (1994) Medical microbiology-illustrated. Butterworth Heinemann, London, pp 234–237Google Scholar
- 21.Idhayadhulla A, Surendra Kumar R, Jamal Abdul Nasser A (2011) Synthesis, characterization and antimicrobial activity of new pyrrole derivatives. J Mex Chem Soc 55:218–223Google Scholar