Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors

…, EMM de la Nava, DR Mayhugh, SL Cockerham…

Index: Escribano, Ana; Mateo, Ana I.; Martin De La Nava, Eva M.; Mayhugh, Daniel R.; Cockerham, Sandra L.; Beyer, Thomas P.; Schmidt, Robert J.; Cao, Guoqing; Zhang, Youyan; Jones, Timothy M.; Borel, Anthony G.; Sweetana, Stephanie A.; Cannady, Ellen A.; Mantlo, Nathan B. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3671 - 3675

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Citation Number: 5

Abstract

Our research program is based on identifying orally active CETP inhibitors. Along with other groups, 10 we focused our attention on exploring the tetrahydroquinoline scaffold. This communication describes structure–activity relationship studies of tetrazoyl derivatives 6. Subsequent optimization was undertaken, leading to the discovery of several analogues that significantly raised HDL-c in a double transgenic mouse model expressing human CETP and apolipoprotein ...