Synthesis and Antibacterial Activity of Lactivicin Derivatives
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概要
- 論文の詳細を見る
The chemical modification of the 4-acetylamino group on the cycloserine moiety of lactivicin (1a) was carried out.The lactivicin derivatives (1d, k-p and w) having heterocyclic acylamino groups which have been often utillized in β-lactam antibiotics showed potent antibacterial activities. Ester prodrugs (7a-d) of lactivicin derivatives were also prepared in order to improve the bioavailability on oral administration. The pivaloyloxymethyl (POM) esters (7a and 7b) and 1-ethoxycarbonyloxyethyl (EOE) ester (7c) were found to have slightly improved protective effect in vivo compared with their parent compounds 1c and 1k.
- 公益社団法人日本薬学会の論文
- 1990-01-25
著者
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吉岡 晃一
Research And Development Division Takeda Chemical Industries Ltd.
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川野 泰彦
Pharmaceutical Research Division Pharmaceutical Research Laboratories Iii Takeda Chemical Industries
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田村 典一
武田薬品工業(株)
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田村 典一
Research and Development Division, Takeda Chemical Industries, Ltd.,
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松下 義弘
Research and Development Division, Takeda Chemical Industries, Ltd.,
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川野 泰彦
Research and Development Division, Takeda Chemical Industries, Ltd.,
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松下 義弘
Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries
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川野 泰彦
Research And Development Division Takeda Chemical Industries Ltd.
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