Design, Synthesis, and In Vitro Anti-mycobacterial Evaluation 1H-1,2,3-triazole-tethered Ciprofloxacin and Isatin Conjugates

作者：Hu, Yuan-Qiang^*; Meng, Ling-Dan; Qiang, Min; Song, Xu-Feng^*

来源：Journal of Heterocyclic Chemistry, 2017, 54(6): 3725-3729.

DOI：10.1002/jhet.2933

• MYCOBACTERIUM-TUBERCULOSIS
• DERIVATIVES
• AGENTS

Eight novel 1H-1,2,3-triazole-tethered ciprofloxacin (CPFX) isatin conjugates 5a-h with greater lipophilicity compared with CPFX were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activity against Mycobacterium smegmatis and Mycobacterium tuberculosis (MTB) H(37)Rv. The preliminary results showed that all hybrids (MIC: 12.5-100 mu g/mL) exhibited considerable activity against M. smegmatis, but less active than the parent CPFX (MIC: 6.25 mu g/mL) and the reference INH (MIC: 0.78 mu g/mL). Against MTB H37Rv, all hybrids displayed excellent inhibitory activity with MICs ranging from 1.56 to 25 mu g/mL, particularly, 5h (MIC: 1.56 mu g/mL) was twofold more active CPFX (MIC: 3.12 mu g/mL), warrant further investigations.

• 出版日期2017-11
• 单位北京工业大学; 湖北工程学院; 武汉大学; 武汉科技大学