Synthesis, Characterization and Antibacterial Activity Study of Para‐substituted Derivatives of N ‐benzyl‐3‐methylbuten‐2‐enamides

Abstract In order to deeply explore the effect of para‐substituents on the antibacterial activity of N ‐benzyl‐3‐methylbuten‐2‐ enamide derivatives, we elaborately synthesized three such para‐substituted derivatives (compound a : N ‐(4‐hydroxybenzyl)‐3‐methylbut‐2‐ enamide; compound b : N ‐(4‐isobutoxybenzyl)‐3‐ methylbut‐2‐enamide; compound c : N ‐(4‐isopropoxybenzyl) −3‐methylbut‐2‐ enamide), of which the structures were determined by ways of single crystal X‐ray diffraction data analysis mainly. The antibacterial performance experiments showed that compounds a , b and c were evaluated for their antibacterial ( Escherichia coli , Staphylococcus aureus, and Enterobacter aerogenes ) activities. Among them, compounds a , b and c have an effective antibacterial reagents for E. coli exhibiting MIC values of 0.01, 0.01 and 0.01 g/mL, respectively, but inactive for E. aerogenes . In addition, compounds b and c have better activity than compound a against S. aureus with MIC values of 0.01 and 0.02 g/mL. These results provide an important basis for further study of the antibacterial properties and structure‐activity relationship of these compounds, and are expected to provide valuable reference for the development of new antibacterial drugs.