📗 A facile method has been implemented for the synthesis of different N-substituted sulfamoylacetamides (3a-q) by the reaction of 4-acetamidobenzenesulfonyl chloride with a series of different alkyl/aralkyl/aryl amines in aqueous alkaline media under dynamic control of pH at 9-10. The structures of the synthesized N-substituted sulfamoylacetamides were elucidated through spectral analysis like FT-IR, EIMS and 1H-NMR. The synthesized derivatives were further screened against Chymotrypsin enzyme. The results revealed that most of the synthesized compounds were found to be potent chymotrypsin inhibitor.