1<i>H</i>‐1,2,3‐triazole‐tethered 8‐OMe Ciprofloxacin and Isatin Hybrids: Design, Synthesis and <i>in vitro</i> Anti‐mycobacterial Activities

Abstract

A new class of 1 H ‐1,2,3‐triazole‐tethered 8‐OMe ciprofloxacin (8‐OMe CPFX) isatin hybrids 5a–l was designed, synthesized and screened for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H 37 Rv and multi‐drug‐resistant tuberculosis (MDR‐TB). All targets (minimum inhibitory concentration (MIC): 0.20–8.0 μg/mL) exhibited promising inhibitory activity against MTB H 37 Rv and MDR‐TB. Among them, conjugate 5h (MIC: 0.20 μg/mL), was 2–16 times more potent in vitro than the references CPFX (MIC: 3.12 μg/mL), 8‐OMe CPFX (MIC: 1.56 μg/mL) and RIF (MIC: 0.39 μg/mL) against MTB H 37 Rv. The most potent hybrid 5l (MIC: 0.25 μg/mL) was 8–256 times more active than the three references (MIC: 2.0–64 μg/mL) against MDR‐TB. Both of them warrant further investigations.