論文 - 詳細
RRC ID | 60542 |
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著者 | Ishizaki Y, Takahashi Y, Kimura T, Inoue M, Hayashi C, Igarashi M. |
タイトル | Synthesis and biological activity of analogs of CPZEN-45, a novel antituberculosis drug. |
ジャーナル | J Antibiot (Tokyo) |
Abstract |
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. |
巻・号 | 72(12) |
ページ | 970-980 |
公開日 | 2019-12-1 |
DOI | 10.1038/s41429-019-0225-5 |
PII | 10.1038/s41429-019-0225-5 |
PMID | 31471594 |
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 |
IF | 2.446 |
引用数 | 1 |
リソース情報 | |
一般微生物 | JCM6384 |