title: Carbohydrate modifications in the spirostane cellobioside cholesterol absorption inhibitor series.
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.
authors.affiliation: Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
authors.forename: M P
authors.initials: MP
authors.lastname: DeNinno
authors.forename: C
authors.initials: C
authors.lastname: Eller
authors.forename: J B
authors.initials: JB
authors.lastname: Etienne
mesh_terms: D000924:Anticholesteremic Agents / Q000737:chemistry* / Q000494:pharmacology; D002475:Cellobiose / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D013150:Spirostans / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000924:Anticholesteremic Agents; D013150:Spirostans; D002475:Cellobiose