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

Author(s): Coppola GM, Damon RE, Eskesen JB, France DS, Paterniti JR Jr

Affiliation(s): Department of Diabetes and Metabolism, Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA. gary.coppola@novartis.com

Publication date & source: 2006-01-01, Bioorg Med Chem Lett., 16(1):113-7. Epub 2005 Oct 10.

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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