CARBOHYDRATE MODIFICATIONS IN THE SPIROSTANE CELLOBIOSIDE CHOLESTEROLABSORPTION INHIBITOR SERIES

Cholesterol absorption inhibition remains an attractive approach for t he treatment of hypercholesterolemia. We have continued our SAR develo pment in the spirostanyl cellobioside class of agents seeking a greate r 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 thi s study, it was determined that the minimal requirements for optimal p otency was a lone carbamate at C4 '' and deoxygenation at the C6 '' po sition, (C) 1998 Elsevier Science Ltd. All rights reserved.