Reference - Detail
|Author||Ishizaki Y, Takahashi Y, Kimura T, Inoue M, Hayashi C, Igarashi M.|
|Title||Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug.|
|Journal||J Antibiot (Tokyo)|
Analogs of CPZEN-45, which is expected to be a promising new antituberculosis drug that overcomes the shortcomings of caprazamycins, were synthesized and their biological activities were evaluated. The biological activity of analogs 1-3, which converted the anilide portion, and analogs 4 and 5, focusing on the seven-membered ring, were lower than that of CPZEN-45. These results suggest that the inhibitory activity of CPZEN-45 against TagO, an ortholog of WecA, has a strict structural limitation, and it was hoped for elucidation of the mode of action of CPZEN-45 using structural biology in the future.
|MeSH||Antitubercular Agents / chemical synthesis* Antitubercular Agents / chemistry Antitubercular Agents / pharmacology* Azepines / chemistry* Bacillus subtilis / drug effects Bacillus subtilis / enzymology Bacillus subtilis / genetics Bacterial Proteins / antagonists & inhibitors Bacterial Proteins / genetics Bacterial Proteins / metabolism Escherichia coli Proteins / antagonists & inhibitors Microbial Sensitivity Tests Molecular Structure Mycobacterium / drug effects* Structure-Activity Relationship* Transferases / antagonists & inhibitors Transferases / genetics Transferases / metabolism Transferases (Other Substituted Phosphate Groups) / antagonists & inhibitors|