PUBLICATION
Evaluation the anti-Mycobacterial activity of newly synthesized (S)-N-(3-(2-fluoro-4'-(2-amino-4-thiazolyl)biphenyl-4-yl)-2-oxo-1,3-oxazolidie-5-ylmethyl) acetamide derivative in vitro and in Mycobacterium marinum infected zebrafish
- Authors
- Ding, X., Wu, Y., Tong, A., Sun, B., Zhao, Y., Jiang, Y.
- ID
- ZDB-PUB-201103-5
- Date
- 2020
- Source
- Japanese journal of infectious diseases 74(3): 245-248 (Journal)
- Registered Authors
- Keywords
- Linezolid, MmIZ model, anti-Mycobacterial activities, oxazolidinones
- MeSH Terms
-
- Acetamides/pharmacology*
- Animals
- Anti-Bacterial Agents/pharmacology*
- China
- Microbial Sensitivity Tests
- Mycobacterium Infections, Nontuberculous/drug therapy*
- Mycobacterium marinum/drug effects*
- Oxazolidinones/pharmacology*
- Zebrafish
- PubMed
- 33132296 Full text @ Jpn J Infect Dis
Citation
Ding, X., Wu, Y., Tong, A., Sun, B., Zhao, Y., Jiang, Y. (2020) Evaluation the anti-Mycobacterial activity of newly synthesized (S)-N-(3-(2-fluoro-4'-(2-amino-4-thiazolyl)biphenyl-4-yl)-2-oxo-1,3-oxazolidie-5-ylmethyl) acetamide derivative in vitro and in Mycobacterium marinum infected zebrafish. Japanese journal of infectious diseases. 74(3):245-248.
Abstract
Our previous work have identified a novel oxazolidinones structure, biaryloxazolidinone analogues containing a hydrazone moiety, as promising antibacterial agents against Gram positive strains. Based on these active structure, we synthesized a series novel oxazolidinones here and determine their anti-Mycobacterial activities in vitro and in Mycobacterium marinum (M.marinum) infected Zebra fish. The in vitro anti-Mycobacterial assay demonstrated that all of them have potent efficacy against both H37Rv and clinical Mycobacterial isolates. Among of these active agents, (S)-N-(3-(2-fluoro-4'-(2-amino-4-thiazolyl)biphenyl-4-yl)-2-oxo-1,3-oxazolidie-5-yl methyl)acetamide (compound 7), whose in vitro MIC was 10 fold lower than linezolid, showed the strongest bactericidal effects, with ~2.2 log reduction of M.marinum load in Zebra fish at 10mg/kg. Other novel oxazolidinones, compound 9, 12, 16, and 21 showed reduction range against M.marinum at 1.1-1.8 log, which showed better efficacy than linezolid did. Our results indicate that these identified compounds could be further developed as novel anti-Mycobacterial agents.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping