The sulfonamide functional group has aroused interest in both medicinal and bioorganic chemistry. In this study, some new phenylselanyl–1–(toluene-4 sulfonyl)-1H-tetrazole derivatives (2a–f) have been synthesized using dicyclohexylcarbodiimide/dimethylaminopyridine (DCC/DMAP). The structures of the presently synthesized compounds were elucidated by spectroscopic methods [Fourier-transform infrared (FTIR) spectroscopy, 1 H nuclear magnetic resonance (NMR), 13C nuclear magnetic resonance-attached proton test (13C NMR-APT), and mass spectrometry (MS)]. In addition, the antimicrobial activity of the synthesized compounds and two antibiotics [sulfamethoxazole (SMX) and sulfamerazine (SRZ)] were investigated against some microorganisms.