摘要 |
<p>Castanospermine mono- and di-esters and glycosides of formula <CHEM> wherein R, R' and R" are hydrogen, alkanoyl, cyclohexanecarbonyl, <CHEM> naphthalenecarbonyl optionally substituted by methyl or halogen; phenylalkanoyl wherein the phenyl is optionally substituted cinnamoyl; pyridinecarbonyl optionally substituted thiophenecarbonyl optionally substituted furancarbonyl optionally substituted or a glycosyl, an O-methylglycosyl or Ac-acylated glycosyl radical containing from 1 to 3 hexose or pentose units with attachment at the 1-position of the glycosyl radical; Y is hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, alkylsulfonyl, alkylmercapto, cyano or dimethylamino; Y' is hydrogen, alkyl, alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, alkyl, alkoxy, or halogen; Ac is benzoyl or alkanoyl; active as inhibitors of carbohydrate digestive enzymes and useful in treating diabetes are described herein. The compounds are prepared by the reaction of castanospermine with an appropriate acid halide or anhydride or with an appropriate glycosyl halide or glycosyl acetimidate under conditions which would favor the isolation of the mono- and di-esterified and glycosylated products.</p> |