Design, synthesis and structure–activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
Copyright policy )Design, synthesis and structure–activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors
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.
- AmeriCorps VISTA United States
- Eli Lilly (United States) United States
Dose-Response Relationship, Drug, Cholesterol, HDL, Cholesterol Ester Transfer Proteins, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, Drug Design, Animals, Humans, Naphthyridines
Dose-Response Relationship, Drug, Cholesterol, HDL, Cholesterol Ester Transfer Proteins, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, Drug Design, Animals, Humans, Naphthyridines
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