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. 1998 Feb 3;8(3):313-8.
doi: 10.1016/s0960-894x(98)00008-0.

Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar

W D Vaccaro  1 , H R Davis Jr
Affiliations

Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: enhanced potency by modification of the sugar

W D Vaccaro et al. Bioorg Med Chem Lett. .

Abstract

A glucuronide conjugate of the potent 2-azetidinone cholesterol absorption inhibitor Sch 58235 was synthesized to confirm the structure of a metabolite isolated from in vivo sources. A series of 2-azetidinone glycosides was prepared via Schmidt trichloroimidate methodology. Enhanced cholesterol absorption inhibition was achieved by modification of the sugar moiety.

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