Synthesis of Novel 3-(Piperazin-1-yl)-1,2-benzothiazole Derivatives and Their Antibacterial Activity

A new library of structurally modified 3-(piperazin-1-yl)-1,2-benzothiazole derivatives have been designed and synthesized through a multi-step procedure. Their structures were characterized by IR, 1H NMR, 13C NMR, and mass spectral technique. The synthesized compounds were evaluated for drug likeness or “drugability” according to Lipinski’s rule of five (RO5). One of the compounds showed two violations, whereas the others complied with RO5. The synthesized compounds were also screened for their antibacterial activity by the agar diffusion method, and three of them were found to be active. One of the compounds showed a good activity against Bacillus subtilis and Staphylococcus aureus with MIC 500 µg/mL. The compound with RO5 violations exhibited almost no antibacterial activity.