Synthesis, Molecular Docking and Biological Evaluation of 2-(2-hydrazinyl)thiazoles as Potential Antioxidant, Anti-inflammatory and Anticancer Agent.
BACKGROUND
Recently, the researcher's have worked on development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we are going to report the synthesized 2-(2-hydrazinyl)thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities studies.


OBJECTIVE
The objective of study was to develop novel antioxidant anti-inflammatory and anti-cancer drugs.


METHODS
At the outset, the condensation of substituted acetophenones 1, thiosemicarbazide 2 and α-haloketones 3 carried out using PEG-400 (20 mL) in the presence of 5 mol% glacial acetic acid to afford thiosemicarbazones intermediate. In furthermore, these thiosemicarbazones were reacted with α-haloketones 3 to obtain appropriate 2-(2-hydrazinyl)thiazoles. The synthesized compounds were in vitro tested for their antioxidant, anti-inflammatory, and anti-cancer activity.


RESULTS
In vitro evaluation report showed that nearly all molecules possessed potential antioxidant activity against 2,2-Diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide radical (SOR) and hydrogen peroxide (H2O2) radical scavenging activity. Most of 2-(2-hydrazinyl)thiazoles derivatives have shown significant anti-inflammatory activity as compared to with diclofenac sodium as a reference standard. 2-(2-Hydrazinyl)thiazoles derivatives showed significant anticancer activity for human leukemia cell line K-562 compared to Adriamycin as a reference standard.


CONCLUSION
All tested compounds showed potential 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) radical scavenging activity. Among the tested series, 4b, 4d and 4e exhibited good hydrogen peroxide and 4b, 4e, 4f and 4g showed excellent superoxide radical scavenging activity. In addition, the 4b, 4e and 4g compounds revealed potent in vitro anti-inflammatory activity against standard diclofenac sodium drug. 2-(2-Hydrazinyl)thiazole derivatives such as 4c and 4d showed significant anticancer activity against human leukemia cell line K-562. Thus, these molecules provide an interesting template for design and development new antioxidant, anti-inflammatory and anti-cancer agents.