Key result
Compound 12, a potent and selective CETP inhibitor, demonstrated in vivo efficacy for raising HDL-C comparable to torcetrapib in animal models.
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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.
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Kuo et al. (2009) studied this question. (2R,αS)-3,4-Dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-α-(trifluoromethyl)-1(2H)-quinolineethanol (compound 12) vs. Torcetrapib was evaluated on Raising HDL-C. Compound 12, a potent and selective CETP inhibitor, demonstrated in vivo efficacy for raising HDL-C comparable to torcetrapib in animal models.
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