Nucleosides, nucleotides & nucleic acids · 2020
Synthesis of new uracil derivatives and their sugar hydrazones with potent antimicrobial, antioxidant and anticancer activities.
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Nassar Ibrahim F, Farargy Ahmed F El, Abdelrazek Fathy M, Hamza Zeinab
Аннотация
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.
Предметные рубрики MeSH
Anti-Bacterial AgentsAntifungal AgentsAntineoplastic AgentsAntioxidantsAspergillus flavusBacillus cereusBiphenyl CompoundsCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHep G2 CellsHumansHydrazonesListeria monocytogenesMCF-7 CellsMicrobial Sensitivity TestsMolecular StructurePicratesSalmonellaStaphylococcus aureusStructure-Activity RelationshipSugarsTumor Cells, CulturedUracilYersinia enterocolitica