1H‐1, 2, 3‐triazole‐tethered 8‐OMe Ciprofloxacin and Isatin Hybrids: Design, Synthesis and in vitro Anti‐mycobacterial Activities. (8th September 2017)

• Record Type: Journal Article
• Authors: Xu, Zhi; Song, Xu‐Feng; Qiang, Min; Lv, Zao‐Sheng
• Is Part Of: Journal of heterocyclic chemistry. Volume 54:Number 6(2017:Nov.)
• Page Start: 3735
• Page End: 3741
• Publication Date: 2017-09-08
• Subjects: Heterocyclic compounds -- Periodicals; 547.59
• DOI: 10.1002/jhet.2980
• Languages: English
• ISSNs: 0022-152X

Abstract

Abstract : A new class of 1 H ‐1, 2, 3‐triazole‐tethered 8‐OMe ciprofloxacin (8‐OMe CPFX) isatin hybrids5a–l was designed, synthesized and screened for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H37 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 H37 Rv and MDR‐TB. Among them, conjugate5h (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 H37 Rv. The most potent hybrid5l (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. Abstract :