Design and Synthesis of a Series of 3-Aminobenzenesulfonamide Derivatives and Their Screening for Antimicrobial and Cytotoxic Activity

A series of 3-aminobenzenesulfonamide derivatives with a 3-N-substituted side chains that contain ureas, thioureas or cyclic amines was designed, synthesized and assayed for antibacterial, anti-candidal and cytotoxic activity. The synthesized compounds exhibited minimal antibacterial activity but showed good anti-candidal activity, especially compounds 2a, 2d, 2e, 3a, 3d, 4b, 4c, 4d, 4j, 4k, 4l and 4m with MIC values ranging from 16-64 µg/mL. The thiourea and urea (compounds 2a-f and 3a-d), but not the cyclic amine derivatives (compounds 4a-m), exhibited significant cytotoxic activity against brine shrimp