論文 - 詳細
| RRC ID | 29295 |
|---|---|
| 著者 | Takahashi Y, Igarashi M, Miyake T, Soutome H, Ishikawa K, Komatsuki Y, Koyama Y, Nakagawa N, Hattori S, Inoue K, Doi N, Akamatsu Y. |
| タイトル | Novel semisynthetic antibiotics from caprazamycins A-G: caprazene derivatives and their antibacterial activity. |
| ジャーナル | J Antibiot (Tokyo) |
| Abstract |
Acidic treatment of a mixture of caprazamycins (CPZs) A-G isolated from a screen of novel antimycobacterial agents gave caprazene, a core structure of CPZs, in high yield. Chemical modification of the resulting caprazene was performed to give its various derivatives. The structure-activity relationships of the caprazene derivatives against several mycobacterial species and pathogenic Gram-positive and Gram-negative bacteria were studied. Although caprazene showed no antibacterial activity, the antibacterial activity was restored for its 1'''-alkylamide, 1'''-anilide and 1'''-ester derivatives. Compounds 4b (CPZEN-45), 4d (CPZEN-48), 4f and 4g (CPZEN-51) exhibited more potent activities against Mycobacterium tuberculosis and M. avium complex strains than CPZ-B. These results suggest that caprazene would be a good precursor from which novel semisynthetic antibacterial antibiotics can be designed for the treatment of mycobacterial diseases such as tuberculosis and M. avium complex infection. |
| 巻・号 | 66(3) |
| ページ | 171-8 |
| 公開日 | 2013-3-1 |
| DOI | 10.1038/ja.2013.9 |
| PII | ja20139 |
| PMID | 23532021 |
| MeSH | Anti-Bacterial Agents / chemical synthesis Anti-Bacterial Agents / chemistry Anti-Bacterial Agents / pharmacology* Azepines / chemical synthesis Azepines / chemistry Azepines / pharmacology* Gram-Negative Bacteria / drug effects Gram-Positive Bacteria / drug effects Lipids / chemical synthesis Lipids / chemistry Lipids / pharmacology* Mycobacterium avium / drug effects Mycobacterium tuberculosis / drug effects Nucleosides / chemical synthesis Nucleosides / chemistry Nucleosides / pharmacology* Structure-Activity Relationship Uridine / analogs & derivatives* Uridine / chemical synthesis Uridine / chemistry Uridine / pharmacology |
| IF | 2.668 |
| 引用数 | 41 |
| WOS 分野 | PHARMACOLOGY & PHARMACY BIOTECHNOLOGY & APPLIED MICROBIOLOGY MICROBIOLOGY IMMUNOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 6 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| 一般微生物 | JCM 6384 |