Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents

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.