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Abstract The present work is aiming to the use of 2-hydroxynicotinonitrile in the synthesis of some new pyridine scaffolds and screening their antibacterial activity against a range of Gram-positive and Gram-negative bacteria and anticancer activity. Biological activity of the synthesized pyridine scaffolds- Antibacterial activity of newly synthesized pyridine scaffolds:The newly synthesized pyridine-based compounds were screened for their in vitro antibacterial activity against Gram-positive bacterium (Staphylococcus aureus) and Gram-negative bacterium (Escherichia coli) by the agar diffusion method. The results for antibacterial activities and revealed that there are significant differences in the diameter of inhibition zones. Among the tested compounds, thieno[2,3-b]-pyridine scaffold 15c, substituted with ethyl carboxylate moiety at the second position, displayed excellent antibacterial property against E. Coli (inhibition zone = 25 mm) and S. aureus (inhibition zone = 26 mm). It was even more active than the standard inhibitor (Ampicillin), which inhibits bacteria with inhibition zones 24 mm and 26 mm, respectively. - Cytotoxicity assay: Some of the constructed pyridine scaffolds were evaluated in vitro for their anticancer activity via the standard MTT method versus two human cancer cell lines: HepG2 (hepatocellular carcinoma) and MCF-7 (mammary gland breast cancer). DOX (Doxorubicin) was used as a reference drug for the anticancer activity.Our results (table 2) indicated that the synthesized thieno[2,3-b]-pyridine scaffold 15c, substituted with ethyl carboxylate moiety at the second position, exhibited very strong cytotoxicity against HepG2 and MCF-7 cells. The IC50 values (IC50 = 6.39±0.5) and (IC50 = 5.25±0.4) were very close to the reference drug (Doxorubicin, IC50 = 4.30±0.3 µM). |