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Abstract
Numbers of biologically active compounds are glycosides. Sometimes, the glycosidic
residue is crucial for their activity, in other cases glycosylation only improves
pharmacokinetic parameters. Recent developments in molecular glycobiology brought
better understanding to the aglycone vs. glycoside activities, and made possible to
develop new, more active or more effective glycodrugs based on these findings - very
illustrative recent example is the story of vancomycin. This paper deals with an array
of glycosidic compounds currently used in medicine but also with biological activity
of some glycosidic metabolites of the known drugs. It involves glycosides of vitamins,
polyphenolic glycosides (flavonoids), alkaloid glycosides, glycosides in the group
of antibiotics, glycopeptides, cardiac glycosides, steroid and terpenoid glycosides
etc. The physiological role of the glycosyl and structure-activity relations (SAR)
in the glycosidic moiety (-ies) are discussed.