Bezafibrate Scaffold Derived Hydrazide-Hydrazones: Synthesis and Antioxidant Activities

Abstract

A NEW series of Bezafibrate derived hydrazide-hydrazone analogues were generated by using some five membered, fused heterocyclic and aromatic aldehydes. All the hydrazones were obtained in good yields from methanol at 60-80 °C for 5-8 hours stirring. Moreover, the compounds were also screened for their anti-oxidant activity potentiality at four different concentrations using DPPH method. Among these compounds, compound 6k analogue of bezafibrate was found to be the most active at all the tested concentrations (≈ 40% inhibition at 25 μg/mL) followed by 6j (4-hydroxy, 3-methoxy 5-bromo analogue ≈ 35% at 25 μg/mL) compared to standard ascorbic acid (49.6% at 25 μg/mL).

The N-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish Tg(fli1: EGFP) Model

“…The review of scientific literature proved a wide range of potential applications and beneficial therapeutic effects of compounds containing hydrazone moiety, like hydrazidehydrazones or sulphonyl hydrazones [11,13,15,16,18]. The results of much research, including those carried out by our research group, indicated that molecules containing hydrazone moiety are cytotoxic and cytostatic towards neoplastic cells [18,22,23].…”

“…These substances are also distinguished by numerous properties which are important from the medical and pharmaceutical point of view. The biological activity of compounds from sulphonyl hydrazone and hydrazide-hydrazone group described so far includes antimicrobial, anti-tuberculosis, anti-HIV, anticonvulsant, analgesic, anti-inflammatory, antioxidant, antidepressant, and most importantly, from the point of view of this work-anticancer activity [9][10][11][12][13][14][15][16][17]. In our recently published study, the newly-synthesized benzenesulphonyl hydrazones demonstrated the antiproliferative potential towards three human cancer cell lines: renal cell carcinoma (769-P), liver cancer (HepG2) and lung squamous cell carcinoma (H2170).…”

Synthesis of Novel Gabapentin Scaffold Derived Hydrazide-hydrazones for Potential Antimicrobial agents and Antioxidants

“…To the best of our knowledge, this is the first report in experimenting with carboxylic acid functionality in the GBP scaffold. Further, the authors have also previously reported some antibacterial [16,17] and antioxidant [18] hydrazide-hydrazone molecules. In continuation to it, authors have explored antimicrobial activities of the novel gabapentin hydrazide-hydrazone analogues along with antioxidant activity of interest.…”