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Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors |
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| Affiliation: | 1. REQUIMTE/UCIBIO, Departamento de Química e Bioquímica da Universidade do Porto, Rua do Campo Alegre, 4169-007 Porto, Portugal;2. REQUIMTE/LAQV, Departamento de Química e Bioquímica da Universidade do Porto, Rua do Campo Alegre, 4169-007 Porto, Portugal;3. Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, E-15782 Santiago de Compostela, Spain |
| Abstract: | A series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein with aminoheterocycles appended onto the N-terminus of the chemotype were explored as urea mimetics. Potent compounds were discovered and were further optimized to improve metabolic stability and PXR transactivation profile. |
| Keywords: | CETP |
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