Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592448 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
This Letter describes the discovery and SAR optimization of 1,5-tetrahydronaphthyridines, a new class of potent CETP inhibitors. The effort led to the identification of 21b and 21d with in vitro human plasma CETP inhibitory activity in the nanomolar range (IC50Â =Â 23 and 22Â nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Maria-Carmen Fernandez, Ana Escribano, Ana I. Mateo, Saravanan Parthasarathy, Eva M. Martin de la Nava, Xiaodong Wang, Sandra L. Cockerham, Thomas P. Beyer, Robert J. Schmidt, Guoqing Cao, Youyan Zhang, Timothy M. Jones, Anthony Borel,