Synthesis of novel thiazole derivatives linked benzonitrile moiety as potent antimicrobial agents.

Aim

This study aims to design a new series of thiazoles by combining a thiazole core with a benzonitrile moiety via a suitable linker. Additionally, a hydrazone linker was employed to enhance molecular flexibility and facilitate favorable interactions within the DNA gyrase active site and testing their antimicrobial.

Materials And Methods

We synthesized a series of thiazole‑linked benzonitrile moiety through the reaction of thiosemicarbazone derivative with α-halocarbonyl reagents in basic refluxing dioxane. The novel derivatives were investigated for their antimicrobial activity.

Results

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Conclusion

All derivatives showed excellent inhibition toward the used bacteria with inhibition zone diameter ranging from 10 to 35 mm. The evaluated thiazole derivatives exhibited superior antibacterial activity compared to antifungal activity, as none demonstrated efficacy against Aspergillus niger. Several derivatives showed antibacterial activity exceeded the reference drugs. Moreover, three derivatives 9, 13e, and 13h showed the same low values of both minimum inhibition concentration and minimum bactericidal concentration with Klebsiella pneumoniae, Staphylococcus aureus and Bacillus subtilis. Moreover, the most active derivative 13e exhibited a notable noncytotoxic effect on WI-38 cells revealing its safety. Finally, we have successfully synthesized nontoxic, antibacterial derivatives. Further research on these derivatives is possible to develop an effective antimicrobial drug.