Synthesis, Characterization, Genotoxicity Assessment and Biological Activity of Derivatives Derived from Flucytosine Drug

Because pyrimidine compounds contain two nitrogen atoms in the ring, their structures are a class of significant organic compounds that include hetero atoms. These groups are thought to be the previously derivatives with pharmacological and biological activities toward many types of pathogenic organisms. To study the antimicrobial activity of three different types of derivatives (C1, C2, and C3) against two different species of bacteria (Escherichia coli and Proteus vulgaris) and two different species of fungi (Aspergillus niger and Penicillium chrysogenum), the derivatives have been prepared at three different concentrations (10, 15, and 20 mg/mL). The results showed that three derivatives had antimicrobial activity at all studied concentrations, but the best antibacterial and antifungal effect was recorded at the concentration (20 mg/mL) against all microbial isolates studied. Furthermore, in vivo genotoxicity of two compounds (C2 and C3) was investigated in rats using the 8-hydroxy-20-deoxyguanosine (8-OHdG) assay. In addition, when rats were treated with 500 mg/kg body weight of compound C3, there was a considerable suppression of the urine 8-OHdG level (50.2%) (p < 0.0001). Compound C2, however, raised the amounts of 8-OHdG in the urine. Using an up-and-down method to calculate the fatal dosage (LD50) values for compounds C2 and C3, it was shown that these compounds are safe because the LD50 was greater than 1000 mg/kg" b.w". Because the studied compounds have strong antibacterial activity and low genotoxicity, they may find application as antibiotics.

Synthesis, Characterization, Genotoxicity Assessment and Biological Activity of Derivatives Derived from Flucytosine Drug Keywords:

Pyrimidine , azomethine , Flucytosine drug , Biological activity , genotoxicity