Design, Synthesis and In Vitro Anti-microbial Evaluation of Ethylene/ Propylene-1H-1,2,3-Triazole-4-Methylene-tethered Isatin-coumarin Hybrids
Method: These hybrids were assessed for their in vitro anti-TB activity against MTB H37Rv and MDRTB, as well as anti-bacterial activity against Gram-positive and Gram-negative strains, and cytotoxicity in VERO cell line.
Results: The results showed that all hybrids with acceptable cytotoxicity (CC50: 64-512 μg/mL) exhibited weak to moderate anti-microbial activity. The most active hybrid 8i with MIC of 50 μg/mL against MTB H37Rv and MDR-TB, also has excellent cytotoxicity profile (CC50: 128 μg/mL).
Conclusion: The resistance index of hybrid 8i was 1, indicating that hybrid 8i has no cross-resistance with the first-line anti-TB agent. Thus, hybrid 8i could act as a lead for further optimization.
Document Type: Review Article
Publication date: November 1, 2017
This article was made available online on December 20, 2017 as a Fast Track article with title: "Design, Synthesis and In Vitro Anti-microbial Evaluation of Ethylene/ Propylene-1H-1,2,3-Triazole-4-Methylene-tethered Isatin-coumarin Hybrids".