Synthesis and Antibacterial Activity of Sulfanilamide Derivatives Containing Phosphonate Moiety

In order to find antibacterial candidate agents, using a fragment based drug discovery method, fifteen sulfanilamide derivatives were designed and synthesized with aminophosphonate and sulfonyl chloride as raw material. Their structures were confirmed by IR, 1HNMR and 13CNMR. The minimum inhibitory concentration (MICs) of the target compounds were determined by double dilution method. The results showed that some compounds had potential inhibitory activities against standard bacteria and drug resistant bacteria. The MICs of N-[(diethoxyphosphonyl)-4-fluorobenzyl]-4-methoxybenzenesulfonamide (compound Ⅱf) for Staphylococcus aureus (S. aureus), Escherichia coli (E. coli), Methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Escherichia coli (MREC) were 32, 64, 128, 128 μg/mL, while those of N-[(diethoxyphosphonyl)-4-fluorobenzyl]-4-fluorobenzenesulfonamide (compoundⅡl) were 32, 32, 64, 64 μg/mL against the above mentioned respective strains. Their antibacterial activities were better than that of the control drug sulfadiazine. © 2019, Editorial Office of FINE CHEMICALS. All right reserved.