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Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents
Authors:Coppola Gary M  Damon Robert E  Eskesen J Bruce  France Dennis S  Paterniti James R
Institution:Department of Diabetes and Metabolism, Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA. gary.coppola@novartis.com
Abstract: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. The optimal analogue (HDL376) was shown to raise HDL cholesterol in the rat, hamster, dog, and monkey models.
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