Chemical Biology and Drug Design
Chemical Biology and Drug Design
5 years ago

A Structure-based Strategy toward the Development of Novel Candidates for Antimycobacterial Activity: Synthesis, Biological evaluation and Docking study

A Structure-based Strategy toward the Development of Novel Candidates for Antimycobacterial Activity: Synthesis, Biological evaluation and Docking study
Huiyuan Guo, Zhaoyong Yang, Bin Wang, Yuanyuan Jin, Jun Zhang, Linhu Li, Yu Lu, Mingliang Liu
Bacterial resistance to most of the available antibiotics has stimulated the discovery of novel efficacious antibacterial agents. Bedaquiline is first of its type that has been specifically introduced for the management of MDR-TB in combination with other drugs. In the current study, a series of isoniazid/ethambutol/pyrazinamide -quinoline conjugates based on the structures of Bedaquiline were designed and synthesized. Biological activity tests revealed that some of isoniazid/ethambutol-quinoline conjugates have useful antibiotic activity against MTB H37Rv (MIC: 2.0-8.0μg/mL). Furthermore, molecular docking calculations were performed for the most potent inhibitor to show its binding interactions within the active site of the possible target protein. Overall, these compounds represent novel valuable starting point with potent antimycobacterial activity and deserve further structural modifications. This article is protected by copyright. All rights reserved. In the current study, a series of isoniazid/ethambutol/pyrazinamide -quinoline conjugates based on the structures of Bedaquiline were designed and synthesized. Biological evaluation indicated that some of isoniazid/ethambutol-quinoline conjugates have useful activity against MTB H37Rv (MIC: 2.0-8.0μg/mL).

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.13142

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