Novel 3-O-glycosyl-3-demethylthiocolchicines as ligands for glycine and γ-aminobutyric acid receptors
New 3-O-glycosyl-3-demethylthiocolchicines containing natural and unnatural sugar moieties were prepared and tested on γ-aminobutyric acid (GABA) and strychnine-sensitive glycine receptors present in rat brain and spinal cord. Two different synthetic approaches were used with the readily available 3-O-demethylthiocolchicine (1b) and thiocolchicoside (2a). Glycosyl compounds 2a-g were obtained from 1b and 1-fluorosugars 4. 6′-Heterosubstituted glycosyl compounds 6-12 and the 6′-desoxy derivative 2h were prepared from 2a.
"Process for the glycosidation of colchicine and thiocolchicine"
A process for the preparation of compounds having formula I is disclosed, wherein: - R1 is a methoxy or methylthio group; - R2 is a O-glycosyloxy residue. Compounds having formula I are prepared by reacting the corresponding precursor having R2 = OH and the suitably protected 1-acetyl-glycose.
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(2009/12/23)
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