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Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists |
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| Authors: | Noel Romain Song Xinyi Shin Youseung Banerjee Subhashis Kojetin Douglas Lin Li Ruiz Claudia H Cameron Michael D Burris Thomas P Kamenecka Theodore M |
| Institution: | Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA. |
| Abstract: | The design and synthesis of a novel series of Rev-erbα agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erbα agonists. Through the optimization of the scaffold 1, several potent compounds with good in vivo profiles were discovered. |
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