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