Synthesis, cytotoxicity assessment and antioxidant activity of some new thiazol-2-yl carboxamides,Journal of Heterocyclic Chemistry

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Synthesis, cytotoxicity assessment and antioxidant activity of some new thiazol-2-yl carboxamides
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-05-14 , DOI: 10.1002/jhet.4301
Mamdouh A. Sofan ₁ , Ahmed El‐Mekabaty ₂ , Ali M. Hasel _{1,

3} , Samy B. Said ₁

Affiliation

Dependence on the biological activity of 2-aminothiazole, the synthesis and chemical reactions of ethyl 3-oxo-3-(thiazol-2-ylamino)propanoate (1) with some different reagents were described for cytotoxic and antioxidant evaluation. The new derivatives 2–19 could be synthesized and characterized by correct analytical and spectral data. In addition to the thiazole ring, these compounds contain 2H-1,2,3-triazole (3), 1H-pyrazole (5, 12), 1,3-dithiane (7), benzothiazole (10), thiazolidine (13), thiazolidinone (14, 15), 2H-chromene (17), pyridine (19) moieties. The preparation of compounds 2–19 was performed through the formation of the isolable 2-(2-phenylhydrazineylidene) 2, 2-dimethylaminomethylidene 4, 2-phenylcarbamothioyl 9, 2-(methylthio)(phenylamino) methylidene 11 and non-isolable potassium bis(thiolate) 6, potassium thiolate 8 intermediates from precursor 1. The activity of these derivatives 1–19 against human lung fibroblast (WI38) and human prostate cancer (PC3) were examined in vitro using the MTT assay. The assessment of their antioxidant activities was carried out by following the ABTS method to evaluate their pharmaceutical importance.

中文翻译：

一些新型噻唑-2-基甲酰胺的合成、细胞毒性评估和抗氧化活性

依赖于 2-氨基噻唑的生物活性，描述了 3-oxo-3-(thiazol-2-ylamino)propanoate ( 1 ) 与一些不同试剂的合成和化学反应，用于细胞毒性和抗氧化评估。新的衍生物2-19可以通过正确的分析和光谱数据合成和表征。除了噻唑环外，这些化合物还含有 2 H -1,2,3-三唑 ( 3 )、1 H -吡唑 ( 5 , 12 )、1,3-二噻烷 ( 7 )、苯并噻唑 ( 10 )、噻唑烷 ( 13 ), 噻唑烷酮 ( 14 , 15 ), 2H-色烯 ( 17 )、吡啶 ( 19 ) 部分。通过形成可分离的 2-(2-苯肼亚甲基) 2、2-二甲基氨基亚甲基4、2-苯基氨基甲硫基9、2-(甲硫基)(苯基氨基) 亚甲基11和不可分离的双钾，制备化合物2-19 (硫醇盐) 6 , 硫醇钾8中间体来自前体1。这些衍生物的活性1-19使用 MTT 测定法在体外检查了抗人肺成纤维细胞 (WI38) 和人前列腺癌 (PC3) 的抗性。通过遵循 ABTS 方法来评估它们的抗氧化活性，以评估它们的药学重要性。

更新日期：2021-05-14

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