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

Bioorg Med Chem Lett

Department of Diabetes and Metabolism, Novartis Institutes for Biomedical Research, 100 Technology Square, Cambridge, MA 02139, USA.

Published: January 2006

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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http://dx.doi.org/10.1016/j.bmcl.2005.09.034DOI Listing

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