Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

•We have synthesized a new class of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles.•The pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles compounds show antimicrobial and cytotoxic activity.•The pyrimidinyl bis methylthio benzimidazole showed greater antimicrobial activity than benzoxazole and benzothiazole.

A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly against Staphylococcus aureus (29 mm, MIC 12.5 μg/mL) and Penicillium chrysogenum (38 mm, MIC 12.5 μg/mL). The amino linked pyrimidinyl bis benzothiazole 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 μM.

Graphical abstractA variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound 22 was a potent antimicrobial agent and compound 24 exhibited cytotoxic activity on A549 cells with IC50 value of 10.5 μM.Figure optionsDownload full-size imageDownload as PowerPoint slide