Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592923 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
Several five- and six-membered heterocycles were introduced to replace the C2-position amide bond of the original 2-aminothiazole-based hit compound 5. Specifically, replacement of the amide bond with an imidazolidinone moiety yielded a novel and potent thiazolylimidazolidinone series of SCD1 inhibitors. XEN723 (compound 22) was identified after optimization of the thiazolylimidazolidinone series. This compound demonstrated a 560-fold improvement in in vitro potency and reduced plasma desaturation indices in a dose dependent manner, with an EC50 of 4.5Â mg/kg.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shaoyi Sun, Zaihui Zhang, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Julia Fonarev, Qi Jia, Po-Yee Leung, Jennifer Tran, Leslie G. Ratkay, David G. McLaren, Chris Radomski, Sultan Chowdhury, Jianmin Fu, Brian Hubbard, Michael D. Winther,