Studies of tylosin derivatives effective against macrolide-resistant strains: Synthesis and structure-activity relationships.
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- TSUCHIYA MASAMI
- Institute of Microbial Chemistry
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- HAMADA MASA
- Institute of Microbial Chemistry
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- TAKEUCHI TOMIO
- Institute of Microbial Chemistry
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- UMEZAWA HAMAO
- Institute of Microbial Chemistry
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- YAMAMOTO KENICHI
- Central Research Laboratories, Sanraku-Ocean Co., Ltd.
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- TANAKA HIROSHI
- Central Research Laboratories, Sanraku-Ocean Co., Ltd.
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- KIYOSHIMA KOHKI
- Central Research Laboratories, Sanraku-Ocean Co., Ltd.
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- MORI SHUNRO
- Central Research Laboratories, Sanraku-Ocean Co., Ltd.
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- OKAMOTO ROKURO
- Central Research Laboratories, Sanraku-Ocean Co., Ltd.
書誌事項
- タイトル別名
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- Studies of Tylosin Derivatives Effectiv
- α β
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The 4''-O-substituted tylosin derivatives were prepared by selective esterification of the 4''-OH, and relationships between the substituent groups and antimicrobial activity against macrolide-resistant strains were examined. Introduction of branched-chain aliphatic acyl groups such as 2-methoxyisovaleryl or 4-methylvaleryl group afforded derivatives with good antibacterial activity; MIC values were 12.5 μg/ml against Staphylococcus aureus MS-8710. MIC values of tylosin, erythromycin and josamycin against this strain were 800 μg/ml or more. Further improved activity was obtained by introduction of aromatic groups such as phenylthioacetyl, phenylsulfonylacetyl, 4-nitrophenylacetyl, 4-nitrophenylsulfonyl and phenylethanesulfonyl groups; MIC values were 6.25 μg/ml. These derivatives had also an improved antimycoplasmal activity; MIC values were 0.08μg/ml against macrolide-resistant strains of Mycoplasina gallisepticum. MIC values of tylosin against these strains were from 2.5 to 10μg/ ml. Introduction of the groups described above into the 4''-OH was confirmed to increase the uptake by a resistant strain.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 35 (6), 661-672, 1982
公益財団法人 日本感染症医薬品協会
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詳細情報 詳細情報について
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- CRID
- 1390001204148656640
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- NII論文ID
- 130003409283
- 40005315151
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- NII書誌ID
- AA0069330X
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- COI
- 1:CAS:528:DyaL38XmtFKlsro%3D
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- ISSN
- 18811469
- 00218820
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- NDL書誌ID
- 2491912
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- PubMed
- 7118722
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可