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Synthesis of new uracil derivatives and their sugar hydrazones with potent antimicrobial, antioxidant and anticancer activities
Nucleosides, Nucleotides & Nucleic Acids ( IF 1.1 ) Pub Date : 2020-03-04 , DOI: 10.1080/15257770.2020.1736300
Ibrahim F Nassar 1 , Ahmed F El Farargy 2 , Fathy M Abdelrazek 3 , Zeinab Hamza 4
Affiliation  

Abstract 6-(4-Chloro-3-nitrophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4) was prepared and was reacted with ethyl chloroacetate, hydrazine hydrate, 4-chloroaniline, formaldehyde, acetic anhydride, formic acid, carbon disulfide, 4-cyanobenzaldehyde, triethyl orthoformate, D-sugars, 4-aminoacetophenone, benzoyl choride and cyclohexanone to afford a series of new uracil derivatives (5–18). Examination of some of the prepared compounds for their antimicrobial, antioxidant and anticancer activities was conducted. Among the tested samples, compound 17 was the most active substance against the gram-positive bacteria and was more potent than the reference drug Cefoperazone. Moreover, the antibacterial activity of 17 was higher against gram-negative bacteria. Compounds 6 and 13 reached a higher scavenging ability toward DPPH radicals and are better candidates for antioxidant activity. Also, compounds 6 and 13 had no significant anticancer activity toward liver cancer (Hep G2) and breast cancer (MCF-7) cell lines. Graphical Abstract

中文翻译:

合成新型尿嘧啶衍生物及其具有强效抗菌、抗氧化和抗癌活性的糖腙

摘要 制备了 6-(4-Chloro-3-nitrophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (4) 并与氯乙酸乙酯、水合肼、4 -氯苯胺、甲醛、乙酸酐、甲酸、二硫化碳、4-氰基苯甲醛、原甲酸三乙酯、D-糖、4-氨基苯乙酮、苯甲酰氯和环己酮,以提供一系列新的尿嘧啶衍生物 (5-18)。对一些制备的化合物的抗微生物、抗氧化和抗癌活性进行了检查。在测试的样品中,化合物 17 是对革兰氏阳性菌最有效的物质,并且比参考药物头孢哌酮更有效。此外,17对革兰氏阴性菌的抗菌活性更高。化合物 6 和 13 对 DPPH 自由基具有更高的清除能力,是抗氧化活性更好的候选物。此外,化合物 6 和 13 对肝癌 (Hep G2) 和乳腺癌 (MCF-7) 细胞系没有显着的抗癌活性。图形概要
更新日期:2020-03-04
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