BACKGROUND Recently, researchers have worked on the development of new methods for the synthesis of bioactive heterocycles using polyethylene glycol as a green solvent. In this context, we report the synthesized 2-(2-hydrazinyl) thiazoles for their in vitro antioxidant, in vitro anti-inflammatory and in vitro anti-cancer activities. OBJECTIVE The objective of the 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 was carried out using PEG-400 (20 mL) in the presence of 5 mol% glacial acetic acid to afford thiosemicarbazones intermediate. 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 2-(2-hydrazinyl) thiazoles derivatives have shown potential anti-inflammatory activity as compared to 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 the design and development of new antioxidant, anti-inflammatory, and anti-cancer agents.

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2-(2-肼基)噻唑作为潜在抗氧化剂、抗炎剂和重要抗癌剂的合成、分子对接和生物学评价。

背景技术近来，研究人员致力于开发使用聚乙二醇作为绿色溶剂合成具有生物活性的杂环化合物的新方法。在这方面，我们报告了合成的 2-(2-肼基) 噻唑的体外抗氧化、体外抗炎和体外抗癌活性。目的 本研究的目的是开发新型抗氧化、抗炎和抗癌药物。方法 首先，在 5 mol% 冰醋酸存在下，使用 PEG-400 (20 mL) 将取代的苯乙酮 1、氨基硫脲 2 和 α-卤代酮 3 缩合，得到缩氨基硫脲中间体。此外，这些缩氨基硫脲与 α-卤代酮 3 反应以获得适当的 2-(2-肼基) 噻唑。合成的化合物在体外测试了它们的抗氧化、抗炎和抗癌活性。结果 体外评估报告显示，几乎所有分子都具有潜在的抗氧化活性，可对抗 2,2-二苯基-1-苦基肼 (DPPH)、一氧化氮 (NO)、超氧自由基 (SOR) 和过氧化氢 (H2O2) 自由基清除活性。与作为参考标准的双氯芬酸钠相比，大多数 2-(2-肼基) 噻唑衍生物已显示出潜在的抗炎活性。与作为参考标准的阿霉素相比，2-(2-肼基)噻唑衍生物对人白血病细胞系 K-562 显示出显着的抗癌活性。结论 所有测试的化合物均显示出潜在的 2,2-二苯基-1-苦基肼 (DPPH) 和一氧化氮 (NO) 自由基清除活性。在测试系列中，4b，4d和4e表现出良好的过氧化氢，4b、4e、4f和4g表现出优异的超氧自由基清除活性。此外，4b、4e 和 4g 化合物显示出对标准双氯芬酸钠药物有效的体外抗炎活性。2-(2-肼基)噻唑衍生物，如 4c 和 4d，对人类白血病细胞系 K-562 显示出显着的抗癌活性。因此，这些分子为设计和开发新的抗氧化剂、抗炎剂和抗癌剂提供了有趣的模板。对人白血病细胞系 K-562 显示出显着的抗癌活性。因此，这些分子为设计和开发新的抗氧化剂、抗炎剂和抗癌剂提供了有趣的模板。对人白血病细胞系 K-562 显示出显着的抗癌活性。因此，这些分子为设计和开发新的抗氧化剂、抗炎剂和抗癌剂提供了有趣的模板。