Relationship between addition reactivity and antibacterial activity of α,β-unsaturated amide derivatives of benzimidazolone

Addition reactivity of α,β-unsaturated amide derivatives of benzimidazolone,compounds Ⅰ-Ⅵ,was determined by reacting with glutathione,and their antibacterial activity against Bacillus cereus was evaluated by micro-broth dilution method,and the relationship between addition reactivity and bioactivity of tested compounds was further investigated.The results indicated that the second-order rate constants(KGSH) of compounds Ⅰ-Ⅴ were ranged from 0.055 9 to 0.063 8 L/(mmol·min),and the KGSH value of the most reactive compound,compound Ⅵ,was 0.290 L/(mmol·min).The minimum inhibitory concentration (MIC) of the most potential compounds, Ⅱ and Ⅵ,were 0.78 μg/mL. The results indicated that addition reactivity of α,β-unsaturated amide derivatives of benzimidazolone may not be used to quantitatively predict their antibacterial activity.