Aminoglycosides semi synthetic

Table 1.19. Some aminoglycoside antibiotics which have gained significant therapeutic application. Producer microorganisms are listed in brackets. In addition to naturally produced aminoglycosides, a number of semi-synthetic derivatives have also found medical application. Examples include amikacin, a semi-synthetic derivative of kanamycin and netilmicin, an N-ethyl derivative of sissomicin...

In spite of the broad antibacterial spectrum of aminoglycosides and their effective utilisation in cases of severe bacterial diseases, world-wide attempts have been made to develop new aminoglycosides with improved properties and reduced side effects. A main goal in the development of new semi-synthetic products has been the selective protection and modification or elimination of the numerous hydroxyl-and amino groups, the exchange of specific aminosugars or aminocyclitols and the introduction of amino acids as in butirosin. 

Products of the oxidative degradation 253, 254), in which the 4-0 attached aminoglycosyl moiety is removed, show less or no activity K. Fujisawa etal. ) studied the structure-toxicity relations of 25 natural and semi-synthetic aminoglycosides. They evaluated the acute, intravenous toxicity [LD50] with the assumption that the acute toxicity is related to the oto- and nephrotoxicity, which are the limiting side effect in clinical use. The results are summarized in Table 11... 

Aminoglycoside and Aminocyclitol Antibiotics Reviews have appeared on new semi-synthetic aminoglycoside antibiotics, with particular reference to habekacin and polydeoxy-... 

Attaching functionalities at the N-1 position of the 2-deoxysfreptamine on kanamycin or neomycin class antibiotics has been shown to be one of the most effective methods against aminoglycoside resistant bacteria. (27-29) This strategy has led to the development of semi-synthetic amikacin that has a AHB group at N-1 position (Figure 1). The synthesis of kanamycin and neomycin... 

A review on semi-synthetic antibiotics invulnerable to enzymes of resistant bacteria includes references to aminoglycoside derivative. ... 

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