| 摘要 |
New derivatives of 1,3-thiazolidin-4-yl carboxylic acid of the general formula I <IMAGE> (I) wherein R represents hydrogen, (C1-4)alkyl, aralkyl, phenyl, phenyl substituted by a halogen atom or a methoxy group, formyl, acyl, trimethylsilyl; R' represents hydrogen, a pharmaceutically acceptable inorganic or organic cation, (C1-4)alkyl, 2,2,2-trichloroethyl, acetonyl, benzyl, benzyl substituted by nitro or methoxy, phenyl, nitrophenyl, benzhydryl or trimethylsilyl; R' may also represent a radical capable of providing metabolic activation in vivo selected from acetoxymethyl, pivaloyloxymethyl, phthalidyl, benzoyloxymethyl, 5-indanyl, a group of formula <IMAGE> or a group of formula <IMAGE> in which R'' stands for (C1-4)alkyl, (C5-6)cycloalkyl or aryl; A represents hydrogen, halogen, N3, OH, NH2; or a quaternary N-atom, particularly <IMAGE> (and in this case R' is a negative charge; or a O-CO-NH2 group; or a group of the formula OR'''; O-COR''', NH-CO-R''' or SR''', where R''' is (C1-C4)alkyl, aryl, substituted aryl or a heterocyclic group which can carry lower alkyls; n may be zero or 1. The compounds possess antibacterial utility against microbial infections in man, animals and plants.
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