The aminoglycoside antibiotics contain two important structural features. They are amino sugar portion and centrally placed hexose ring, which is either 2-deoxystreptamine or streptidine.
The
aminoglycoside antibiotics contain two important structural features. They are amino
sugar portion and centrally placed hexose ring, which is either
2-deoxystreptamine or streptidine.
i. The bacterial inactivating enzymes targets C-6 and C-2 position,
and the substitution with methyl group at C-6 increases the enzyme resistance.
ii. Cleavage of
3-hydroxyl or the 4-hydroxyl or both groups does not affect the activity.
i.Various modiļ¬cations at C-1 amino group have been tested. The
acylation (e.g. amikacyn) and ethylation (e.g. 1-N-ethylsisomycin) though does not increase the activity helps to
retain the antibacterial potency.
ii. In sisomicin
series, 2-hydroxylation and 5-deoxygenation result in the increased inhibition
of bacterial inactivating enzyme systems. Thus, very few modiļ¬cations of the
central ring are possible, which do not violate the activity spectrum of
aminoglycosides.
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