Carbohydrate conjugated bio-active compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536124, C07H 100

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active

057235899

ABSTRACT:
Methods and compositions are provided which increase the cellular uptake of bioactive materials by covalently bonding such compounds to carbohydrate moieties through chemical linkers using other than glycosidic bonds. Numerous carbohydrates, linkers and bioactive materials can be joined in this way to form novel compositions, which are collectively referred to herein as glinkosides. Preferred glinkosides are preferentially taken up by glucose receptor and/or other cellular receptors, and once inside the cells, the glinkosides are cleaved into a sugar, a linker or linker fragments, and a biologically active compound. Various aspects of the invention include processes for synthesizing glinkosides, glinkoside compositions, and methods of treating diseases using glinkosides.

REFERENCES:
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Akhtur, S., Routledge, A., Patel, R and Gardiner, J., Synthesis of Mono-and Dimannoside Phosphoramidite Derivatives for Solid-Phase Conjugation to Oligonucleotides, Tetrahedron Letters, 36:40, 7333-7336 (1995).
Molema, G., Jansen, R.W., Pauwells, R., Clerco, E., Meijer, D.K.F., Targeting of Antiviral Drugs to T.sub.4 -Lymphocytes, Biochemical Pharmacology, 40:12, 2603-2610 (1990).

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