867012-52-0Relevant articles and documents
Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
Fernandez, Maria-Carmen,Escribano, Ana,Mateo, Ana I.,Parthasarathy, Saravanan,Martin De La Nava, Eva M.,Wang, Xiaodong,Cockerham, Sandra L.,Beyer, Thomas P.,Schmidt, Robert J.,Cao, Guoqing,Zhang, Youyan,Jones, Timothy M.,Borel, Anthony,Sweetana, Stephanie A.,Cannady, Ellen A.,Stephenson, Gregory,Frank, Scott,Mantlo, Nathan B.
, p. 3056 - 3062 (2012/06/17)
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 (IC50 = 23 and 22 nM, respectively). Both 21b and 21d exhibited robust HDL-c increase in hCETP/hApoA1 dual heterozygous mice model.
