Monocyclic beta-lactam antibiotics: synthesis and antibacterial activity of 4-(substituted ethyl)-2-azetidinone-1-sulfonic acid derivatives |
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Authors: | H Yamashita N Minami K Sakakibara S Kobayashi M Ohno M Hamada H Umezawa |
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Affiliation: | Department of Chemistry, Teikoku Hormone Mfg. Co., Ltd., Kanagawa, Japan. |
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Abstract: | The synthesis and antibacterial activity of sodium (3S,4R)-3-[2-(2-aminothiazol-4-yl)-(Z)-2-(O-substituted oxyimino)acetamido]-2-azetidinone-1-sulfonates having various substituted ethyl groups at the C-4 position are described. Among various substituents explored, the (substituted isothiuronio)ethyl groups were found to have strong antibacterial activity against a variety of Gram-negative bacteria, and moreover, the ethylene isothiuronium derivative exhibited moderate antibacterial activity against Staphylococcus aureus. |
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