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Curr Med Chem. 2001 Sep;8(11):1303-28.

Glycosides in medicine: "The role of glycosidic residue in biological activity".

Author information

1
Institute of Microbiology, Academy of Sciences of the Czech Republic, Laboratory of Biotransformation, Videnská 1083, Prague, CZ-142 20, Czech Republic. kren@biomed.cas.cz

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.

PMID:
11562268
DOI:
10.2174/0929867013372193
[Indexed for MEDLINE]

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