Abstract

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.

中文翻译：

---

新型3-(1-哌嗪基)-1,2-苯并噻唑衍生物的合成及其抗菌活性

摘要

通过多步程序设计并合成了一个新的结构修饰 3-(piperazin-1-yl)-1,2-benzothiazole 衍生物库。它们的结构通过IR、¹ H NMR、¹³ C NMR和质谱技术表征。根据 Lipinski 五法则 (RO5) 评估合成化合物的药物相似性或“成药性”。其中一种化合物显示出两次违规，而其他化合物则符合 RO5。还通过琼脂扩散法筛选了合成的化合物的抗菌活性，发现其中三种化合物具有活性。其中一种化合物对枯草芽孢杆菌和金黄色葡萄球菌表现出良好的活性含 MIC 500 µg/mL。违反 RO5 的化合物几乎没有抗菌活性。