Direct introduction of a formamido group into the 7.ALPHA.(6.ALPHA.)-position of cephalosporins (pencillins).
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- KAMACHI HAJIME
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- OKITA TAKAAKI
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- YAMASAKI TETSURO
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
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- NAITO TAKAYUKI
- Bristol-Myers Research Institute, Ltd., Tokyo Research Center
抄録
A novel direct introduction of a formamido group into the 7α(6α)-position of cephalosporins (penicillins) was achieved by treatment of 7β(6β-[(3, 5-di-tert-butyl-4-oxo-2, 5-cyclohexadien-1-ylidene)methylimino]cephem (penam) esters with N, N-bis(trimethylsilyl)formamide, followed by deblocking with Girard reagent T to give the corresponding 7α(6α)-foimamido-7β(6β-amino derivatives. Three 7α-formamidocephalosporins were prepared by the conventional N-acylation of 7α-formamidocephem. All of them were resistant to β-lactamases, showing similar MIC values against both of a pair of a β-lactamase-producing strain and the corresponding non or low-producing strain of the same species of bacteria, when tested on Staphylococcus aureus, Klebsiella pneurnoniae, Escherichia coli, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Enterobacter cloacae and Citrobacter freundii.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 43 (7), 820-829, 1990
公益財団法人 日本感染症医薬品協会
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キーワード
詳細情報 詳細情報について
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- CRID
- 1390282679124351872
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- NII論文ID
- 130003409955
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- ISSN
- 18811469
- 00218820
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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
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可