U. Valcavi, R. Aveta, A. Brandt, G. Corsi, E. Bosone, P. Farina, G. Guazzi
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引用次数: 0
摘要
以侧链取代α -氧亚胺基团(氮曲南)为模型，通过Z型腙(I a, e)与3-氨基-4-甲基-2-氧-1-叠氮丁磺酸四丁基铵缩合，制备了一系列2-(2-氨基噻唑-4-基)-2-肼-乙酰氨基单巴坦(II a, f)。在这个合成过程中发生了异构化，所有化合物都变成了E型。Monobactams (II a, f)与aztreonam和一些具有相同e -肼侧链的头孢菌素相比，没有明显的体外抗菌活性。
Synthesis and in vitro antibacterial activity of a new series of monobactam derivatives.
Using as a model monobactams with a substituted alpha-oxyimino moiety in the side chain (aztreonam), a series of 2-(2-aminothiazol-4-yl)-2-hydrazono-acetamido monobactam (II a, f) were prepared by condensation of the hydrazones (I a, e) (Z form) with tetrabutylammonium 3-amino-4-methyl-2-oxo-1-azetidin-sulphonate. Isomerization occurred during this synthesis and gave the E form of all compounds. Monobactams (II a, f) showed no significant in vitro antibacterial activity when compared with aztreonam and with some cephalosporins bearing the same E-hydrazono side chain.
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