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Monocyclic beta-lactam antibiotics: synthesis and antibacterial activity of 4-(substituted ethyl)-2-azetidinone-1-sulfonic acid derivatives
Authors:H Yamashita  N Minami  K Sakakibara  S Kobayashi  M Ohno  M Hamada  H Umezawa
Affiliation:Department of Chemistry, Teikoku Hormone Mfg. Co., Ltd., Kanagawa, Japan.
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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