A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzensulfonamides were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Certain compounds inhibit bacterial growth with low MIC (microg/mL) values. The most active compounds 30, 31, and 32 have the lowest MIC values with 0.39 to 0.19 microg/mL. Among the compounds having sulfonamido moities, 16, 23, and 24 exhibited the strongest antibacterial activity with 1.56 microg/mL MIC values.