Design, Synthesis, and Antibacterial Activity of Morpholine-4-sulfonamide Derivatives

Abstract

In the search for novel antibacterial agents, a series of N-(substituted nitrophenyl)morpholine-4-sulfonamides were prepared by the reactions of substituted nitrobenzenes with morpholine-4-sulfonamide under MW irradiation. The synthetic approach is characterized by a facile procedure and broad substrate scope. Preliminary biological assessment of the activity of compounds 1b–1h, 1k–1n against Xanthomonas oryzae pv. oryzae (Xoo) was higher than 80% at 800 μg/mL. Especially, the inhibition rate of compounds 1d, 1k, and 1n were higher than 95%. Significantly, the EC₅₀ value of 1d was close to the sanguinarine.