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Synthesis of Some New Pyrazoline-Based Thiazole Derivatives and Evaluation of Their Antimicrobial, Antifungal, and Anticancer Activities
Russian Journal of Bioorganic Chemistry ( IF 1.1 ) Pub Date : 2020-05-01 , DOI: 10.1134/s1068162020030061
Safaa I. Elewa , Eman Mansour , Ibrahim F. Nassar , Amal A. I. Mekawey

Abstract 3-(2-Thienyl)-5-aryl-1-thiocarbamoyl-2-pyrazolines were reacted with chloroacetone derivatives and hydrazonyl chloride derivatives in ethanol to afford the corresponding thiazolylpyrazoline derivatives and thiophenylpyrazolyl-5-substituted aryl-diazenylthiazole derivatives, respectively. The structures of the newly synthesized compounds were elucidated by different elemental and spectral analyses (IR, mass, 1 H and 13 C NMR). The antimicrobial and antifungal activities of the newly synthesized compounds were evaluated against four bacterial species and five fungal strains. In addition, the antitumor activities of two of the newly synthesized compounds 1-(2-(5-(4-chlorophenyl)-3-(thiophen-2-yl)-4,5-dihydropyrazol-1-yl)-4-methyl thiazol-5-yl)ethan-1-one and 2-(5-(4-chlorophenyl)-3-(thiophen-2-yl)-4,5-dihydro-1 H -pyrazol-1-yl)-4-methyl-5-(phenyl-diazenyl)thiazole against HEPG-2, HCT-116, MCF-7, BHK, and CACO-2 were evaluated. From the obtained results, we found that these two compounds were the most potent candidates towards all gram-positive and gram-negative bacteria, as well as the fungi studied. Also, the same two compounds showed strong antitumor activities against two of the tumor cell lines (HCT-116 and CACO-2).

中文翻译:

一些新型吡唑啉基噻唑衍生物的合成及其抗微生物、抗真菌和抗癌活性的评价

摘要 3-(2-噻吩基)-5-芳基-1-硫代氨基甲酰基-2-吡唑啉与氯丙酮衍生物和腙氯衍生物在乙醇中反应,分别得到相应的噻唑基吡唑啉衍生物和噻吩基吡唑基-5-取代芳基-二烯基噻唑衍生物。新合成化合物的结构通过不同的元素和光谱分析(红外、质谱、 1 H 和 13 C NMR)阐明。针对四种细菌物种和五种真菌菌株评估了新合成化合物的抗菌和抗真菌活性。此外,两个新合成的化合物 1-(2-(5-(4-chlorophenyl)-3-(thiophen-2-yl)-4,5-dihydropyrazol-1-yl)-4-) 的抗肿瘤活性甲基噻唑-5-基)乙-1-酮和2-(5-(4-氯苯基)-3-(噻吩-2-基)-4,5-dihydro-1 H -pyrazol-1-yl)-4-methyl-5-(phenyl-diazenyl)thiazole 对 HEPG-2、HCT-116、MCF-7、BHK 和 CACO-2 进行了评估。从获得的结果中,我们发现这两种化合物是对所有革兰氏阳性菌和革兰氏阴性菌以及所研究的真菌最有效的候选物。此外,同样的两种化合物对两种肿瘤细胞系(HCT-116 和 CACO-2)显示出很强的抗肿瘤活性。
更新日期:2020-05-01
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