Potent glycosidase inhibitors, N-phenyl cyclic isourea derivatives of 5-amino- and 5-amino-1-C-(hydroxymethyl)-cyclopentane-1,2,3,4-tetraols

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

Nine N-phenyl cyclic isourea derivatives of kuninocyclopentanepolyols were prepared conventionally, and assayed for enzyme-inhibitory activity against five sugar hydrolases. Two derivatives derived from lL-(1.2,4,5/3)-5-aminol-C-(hydroxymethyl)cyclopentane-1,2,3,4-tetraol, and two from lD-(1,2,3,5/4)- and DL-(1,4,5/2,3)-5-aminocyclopentane-1,2,3,4-tetraols have been shown to possess strong potency against a-glucosidase and P-galactosidase, respectively.

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