In the present work, novel 5‐((1‐benzyl‐1,2,3‐triazol‐4‐yl)methoxybenzylidene)‐2‐(arylamino)thiazol‐4‐one thiazolone incorporated triazole derivatives have been designed as tyrosinase inhibitors. The compounds were synthesized through click reaction in good yield. Moreover, the antityrosinas activity of the synthesized derivatives was evaluated. In the search for establishing a click copper‐catalyzed azide/alkyne cycloaddition (CuAAC) reaction under strict conditions, in terms of a novel air‐stable, a recyclable and efficient magnetic catalyst was planned for new triazole derivatives as a well‐organized copper iodide supported on the functionalized Fe3O4@SiO2 core‐shell (CuI/Fe3O4@SiO2(TMS‐EDTA) nanoparticles). The engineered nanocatalyst synthesized for the first time and characterized by different methods, including FT‐IR spectroscopy, XRD, FESEM, EDX, TEM, TGA, and BET analysis. The excellent catalytic performance in ethanol with high surface area (351.7 m2g−1) and short reaction time for diverse functional groups (120–200 min), no use of toxic solvents, reusability of the catalyst, and using eco‐friendly conditions are the advantageous of this work. Moreover,the nanocatalyst can be used at least five times without any significant decrease in the yield of the reaction. The thiazolidine‐triazole derivatives 9a, 9c, 9e, and 9 g showed promising tyrosinase inhibitory activity with IC50 values in the range of 5.90–9.81 μM. The compounds were found to be considerably more potent tyrosinase inhibitors than the reference inhibitor kojic acid (IC50 = 18.36 μM).
Background: The main issue is finding the most efficient method in the treatment of cancer in terms of early and accurate diagnostic. One of the most modern diagnostic techniques is imaging methods. The accuracy and detection speed of MRI and CT SCAN are high. Methods: The most important complication of iodinated contrast agents in medical imaging is severe renal toxicity Nephrogenic Systemic Fibrosis (NSF). In order to reduce the cytotoxicity of kidney cells caused by the usage of iodized contrast agents a complex agent should be designed. The two drugs which have been used for the synthesis of this compound are L -lysine amino acid and NAcetyl- Cysteine (NAC). Results: The synthesis of this complex due to two dimer molecules with each other and NAC greatly a helper for an antioxidant activity and L-lysine amino acid helps in drug entry into the cells. However, helping for an antioxidant activity heavily reinforce and eventually will successfully reduce the cytotoxicity. When its exposure to HEK 293 cell line (P<0.05). The reduction in toxicity at the dosage of 100 µM has been showed as the greatest reduction. The amount of renal toxicity was reported 40% in Omniscan. Conclusion: Omniscan was tested when iodinated contrast medium was combined with the synthesized 2NAC-LYS-OMNISCAN complex and the human embryonic kidney 293 (HEK293) cell line. Then, the cytotoxicity was reduced to 10 %. On the other hand, the viability increased from 60 % to 90 %, or in other words, the cytotoxicity was reduced from 40 % to 10 %.
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