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Updated: Aug 1, 2026

Biochemical and Structural Characterization of the Carbohydrate Transport Substrate-binding-protein SP0092
Published on: October 2, 2017
Carbohydrate modifications in the spirostane cellobioside cholesterol absorption inhibitor series
M P DeNinno1, C Eller, J B Etienne
1Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
Abstract:
Cholesterol absorption inhibition remains an attractive approach for the treatment of hypercholesterolemia. We have continued our SAR development in the spirostanyl cellobioside class of agents seeking a greater understanding of the role carbamoyl substitution has on the potency in this series. In this regard, a series of differentially substituted carbamate analogs were made with and without deoxygenations. From this study, it was determined that the minimal requirements for optimal potency was a lone carbamate at C4" and deoxygenation at the C6" position.
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