Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents
作者:Gary M. Coppola、Robert E. Damon、J. Bruce Eskesen、Dennis S. France、James R. Paterniti
DOI:10.1016/j.bmcl.2005.09.034
日期:2006.1
A series of 1-alkyl-3-phenylthiourea analogues were prepared and evaluated as HDL- and Apo A-I-elevating and triglyceride-lowering agents. Several derivatives were superior to gemfibrozil (1). The optimal analogue 8d (HDL376) was shown to raise HDL cholesterol in the rat, hamster, dog, and monkey models. (c) 2005 Elsevier Ltd. All rights reserved.