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Bioorganic & medicinal chemistry letters · 2012

Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists

Romain Noel, Xinyi Song, Youseung Shin, Subhashis Banerjee, Douglas Kojetin, Li Lin, Claudia H Ruiz, Michael D Cameron, Thomas P Burris, Theodore M Kamenecka

Bioorganic & medicinal chemistry letters, 22(11), 3739-42 (2012)

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.