TY  - JOUR
TI  - Synthesis, Characterization and Biological Evaluation of Novel Thiourea Derivatives
AB  - Objective: A new series of 4-[3-(substitutedphenyl)thioureido]-N-(6-chloropyrazin-2-yl)benzenesulfonamide were synthesized from sulfaclozine. 
Methods: All compounds were characterized by IR, 1H-NMR spectroscopic methods and elemental analysis. In addition to the antioxidant activity of the synthesis series, enzyme inhibition activities such as anticholinesterase, tyrosinase, α-amylase and α-glycosidase were determined for the first time in this study. 
Results: According to these biological activity test results, compound 2a in the DPPH, 2c in the ABTS˙+ assay exhibited more antioxidant activity than reference standard. All thiourea derivatives demonstrated good BChE inhibitory activity than galantamine. Among the compounds, 2e and 2f showed the best tyrosinase enzyme inhibition activity, while 2g had the best α-amylase and α-glucosidase enzyme inhibition activity. In addition, we evaluated the druglikeness properties of compounds and their oral bioavailability were also found to be high.
Conclusion: Thiourea derivatives exhibited remarkable antioxidant activity and enzyme inhibition activity against tyrosinase, cholinesterase, α-amylase and α-glucosidase.
AU  - ÇAKIR, CANSEL
AU  - Çam, Dilaycan
AU  - SICAK, Yusuf
AU  - kırpat, mustafa murat
AU  - Tok, Fatih
DO  - 10.33808/clinexphealthsci.1062872
PY  - 2022
JO  - Clinical and Experimental Health Sciences
VL  - 12
IS  - 2
SN  - 2459-1459
SP  - 533
EP  - 540
DB  - TRDizin
UR  - http://search/yayin/detay/532934
ER  -