Synthesis, potent anti-staphylococcal activity and QSARs of some novel 2-anilinobenzazoles

Synthesis and anti-staphylococcal activity of a number of substituted 2-anilinobenzimidazoles, benzothiazoles and benzoxazoles are reported. The anti-staphylococcal activities were evaluated in standard in vitro MIC assay method. While anilinobenzimidazole derivatives 11–45 showed very potent anti-staphylococcal activities (greatest activity with an MIC value of 0.095 μg/mL), none of the 2-anilinobenzothiazoles and benzoxazole derivatives exhibited inhibitory activity. QSAR analysis of the anilinobenzimidazoles was studied on the relationship between the anti-staphylococcal activity (MIC in μg/ml) and extrapolated log kw values.

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