| Literature DB >> 22497761 |
Maria-Carmen Fernandez1, 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, Stephanie A Sweetana, Ellen A Cannady, Gregory Stephenson, Scott Frank, Nathan B Mantlo.
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 (IC(50)=23 and 22nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.Entities:
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Year: 2012 PMID： 22497761 DOI： 10.1016/j.bmcl.2012.03.075
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823