Faculty of Specific Education, Ain Shams University, Abassia, Cairo, Egypt.
Department of Chemistry, Faculty of Science, Zagazig University, Zagazig, Egypt.
Nucleosides Nucleotides Nucleic Acids. 2020;39(7):991-1010. doi: 10.1080/15257770.2020.1736300. Epub 2020 Mar 4.
6-(4-Chloro-3-nitrophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile () 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 (-). Examination of some of the prepared compounds for their antimicrobial, antioxidant and anticancer activities was conducted. Among the tested samples, compound was the most active substance against the gram-positive bacteria and was more potent than the reference drug Cefoperazone. Moreover, the antibacterial activity of was higher against gram-negative bacteria. Compounds and reached a higher scavenging ability toward DPPH radicals and are better candidates for antioxidant activity. Also, compounds and had no significant anticancer activity toward liver cancer (Hep G2) and breast cancer (MCF-7) cell lines.
6-(4-氯-3-硝基苯基)-4-氧代-2-硫代-1,2,3,4-四氢嘧啶-5-甲腈 () 被制备,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、苯甲酰氯和环己酮反应,得到一系列新的尿嘧啶衍生物 (-)。对一些新合成的化合物进行了抗菌、抗氧化和抗癌活性的研究。在所测试的样品中,化合物 对革兰氏阳性菌的活性最强,比参考药物头孢哌酮更有效。此外,化合物 对革兰氏阴性菌的抗菌活性更高。化合物 和 对 DPPH 自由基的清除能力更强,是更好的抗氧化活性候选物。同时,化合物 和 对肝癌 (Hep G2) 和乳腺癌 (MCF-7) 细胞系没有显著的抗癌活性。