2-Alkoxycarbonylaminopyridines: inhibitors of Mycobacterium tuberculosis FtsZ
doi: 10.1093/jac/dkf075
pmid: 12096015
2-Alkoxycarbonylaminopyridines: inhibitors of Mycobacterium tuberculosis FtsZ
Compounds originally designed as putative tubulin inhibitors were tested as antitubercular agents for inhibition of the Mycobacterium tuberculosis analogue of tubulin, FtsZ. Initial screening of 200 2-alkoxycarbonylpyridines found several that inhibited M. tuberculosis growth. Two compounds, SRI-3072 and SRI-7614, inhibited FtsZ polymerization and were equipotent against susceptible and single-drug-resistant strains of M. tuberculosis. In addition, SRI-3072 reduced the growth of M. tuberculosis in mouse bone marrow macrophages. Our results suggest that these types of compound might be developed into antitubercular drugs effective against the current multidrug-resistant strains of M. tuberculosis.
- Southern Research Institute United States
Macrophages, Pteridines, Antitubercular Agents, Bone Marrow Cells, Azepines, Microbial Sensitivity Tests, Mycobacterium tuberculosis, GTP Phosphohydrolases, Cytoskeletal Proteins, Inhibitory Concentration 50, Mice, Bacterial Proteins, Chlorocebus aethiops, Tuberculosis, Multidrug-Resistant, Animals, Carbamates, Vero Cells
Macrophages, Pteridines, Antitubercular Agents, Bone Marrow Cells, Azepines, Microbial Sensitivity Tests, Mycobacterium tuberculosis, GTP Phosphohydrolases, Cytoskeletal Proteins, Inhibitory Concentration 50, Mice, Bacterial Proteins, Chlorocebus aethiops, Tuberculosis, Multidrug-Resistant, Animals, Carbamates, Vero Cells
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