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Design, Synthesis and In Vitro Anti-microbial Evaluation of Ethylene/ Propylene-1H-1,2,3-Triazole-4-Methylene-tethered Isatin-coumarin Hybrids

[ Vol. 17 , Issue. 29 ]

Author(s):

Xiaohong Jin, Yan Xu , Xuhong Yang, Xiuling Chen , Minghu Wu*, Jianguo Guan and Lianshun Feng   Pages 3213 - 3218 ( 6 )

Abstract:


Objective: A new class of ethylene/propylene-1H-1,2,3-triazole-4-methylene-tethered isatincoumarin hybrids 8a-j, integrating three anti-tuberculosis pharmacophores coumarin, isatin and 1,2,3- triazole was designed and synthesized.

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.

Keywords:

Coumarin, 1, 2, 3-triazoleisatin, Hybrid compounds, Anti-bacterial, Anti-tuberculosis activity, Structure-activity relationship.

Affiliation:

College of Pharmacy, Hubei University of Science and Technology, Xianning, State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, International School of Materials Science and Engineering, Wuhan University of Technology, Wuhan, Hubei, School of Nuclear Technology and Chemistry & Life Science, Hubei University of Science and Technology, Xianning, School of Nuclear Technology and Chemistry & Life Science, Hubei University of Science and Technology, Xianning, School of Nuclear Technology and Chemistry & Life Science, Hubei University of Science and Technology, Xianning, State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, International School of Materials Science and Engineering, Wuhan University of Technology, Wuhan, Hubei, Peking University, Beijing

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