The 2-deoxy analogue of 3-deoxy-beta-D-manno-2-octulopyranosonic acid (2-deoxy-beta-KDO, 2) is a potent inhibitor of the enzyme 3-deoxy-D-manno-octulosonate cytidylyltransferase, which is involved in the biosynthesis of lipopolysaccharide, an essential component of the outer membrane of Gram-negative bacteria. Since compound 2 lacks antibacterial activity, a series of 8-substituted derivatives of 2 has been synthesized in an attempt to find enzyme inhibitors suitable for modification as antibacterials. Compounds 9, 11, and 13, in which the 8-hydroxy group of 2 is replaced by F, H, and NH2, respectively, were as potent inhibitors of the enzyme as 2, but were devoid of antibacterial activity, with the exception of the amino acid 13, which showed weak activity against some strains of Salmonella typhimurium.
The carbohydrate polymer in an iron-poly (sorbitol-gluconic acid) complex was prepared by using uniformly labelled 14C-sorbitol or 14C-gluconic acid. The distribution of these complexes 7, 14 and 28 days after administration has been followed in non-anaemic and anaemic rats. Most of the 14C from the labelled complexes was found in the expired CO,, faeces and urine. Twenty-eight days after injection of 14C-labelled FerastraiB, less than 13 % of the given dose of either 14C-sorbitol or 14C-gluconic acid labelled preparation could be found in the body. There was no specific accumulation of l4C in any organ except in the bones, where 3 % of the given dose could be seen 28 days after 14C-gluconic acid labelled Ferastral to both non-anaemic and anaemic animals.Key-words: iron-poly (sorbitol-gluconic acid) complex -FerastralBparenteral iron preparation -14C-labelled polymerdistribution of the polymer
Ferastral: Proceedings of a conference
The placental transfer of an iron‐poly (sorbitol‐gluconic acid) complex, Ferastral®, has been studied. By use of the 59Fe‐, 14C‐sorbitol, and 14C‐gluconic acid labelled complexes it was shown that the passage of the iron moiety is related to foetal need and that only negligible amounts of 14C from either 14C‐sorbitol or 14C‐gluconic acid labelled iron complexes were found in the foetus. This implies that the intact complex does not pass the placental barrier.
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