Design, Synthesis, and Biological Evaluation of (2R,αS)-3,4-Dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-α-(trifluoromethyl)-1(2H)-quinolineethanol as Potent and Orally Active Cholesteryl Ester Transfer Protein Inhibitor

Citations Over TimeTop 10% of 2009 papers

Abstract

With the goal of identifying a CETP inhibitor with high in vitro potency and optimal in vivo efficacy, a conformationally constrained molecule was designed based on the highly potent and flexible 13. The synthetic chemistry efforts led to the discovery of the potent and selective 12. In high-fat fed hamsters, human CETP transgenic mice, and cynomolgus monkeys, the in vivo efficacy of 12 for raising HDL-C was demonstrated to be comparable to torcetrapib.

Related Papers

• → Design, synthesis and molecular simulation studies of dihydrostilbene derivatives as potent tyrosinase inhibitors(2012)41 cited
• → New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation(2013)18 cited
• → Synthesis and SAR studies of a novel class of S1P1 receptor antagonists(2007)14 cited
• → Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 2(2008)11 cited
• → New nonpeptide angiostensin II receptor antagonists. Synthesis, biological properties and structure-activity relationships of 3-substituted 2,6-dialkyl-4-(biphenyll)methylaminopyridine derivatives.(1994)1 cited