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Eur J Med Chem ; 77: 1-7, 2014 Apr 22.
Article in English | MEDLINE | ID: mdl-24607584

ABSTRACT

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.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Benzimidazoles/toxicity , Benzothiazoles/toxicity , Benzoxazoles/toxicity , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Benzimidazoles/chemical synthesis , Benzimidazoles/chemistry , Benzimidazoles/pharmacology , Benzothiazoles/chemical synthesis , Benzothiazoles/chemistry , Benzothiazoles/pharmacology , Benzoxazoles/chemical synthesis , Benzoxazoles/chemistry , Benzoxazoles/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Survival/drug effects , Dose-Response Relationship, Drug , Humans , Microbial Sensitivity Tests , Molecular Structure , Penicillium chrysogenum/drug effects , Staphylococcus aureus/drug effects , Structure-Activity Relationship
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