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ID: ALA1153048

Journal: Bioorg Med Chem Lett

Title: Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.

Authors: Uto Y, Ogata T, Harada J, Kiyotsuka Y, Ueno Y, Miyazawa Y, Kurata H, Deguchi T, Watanabe N, Takagi T, Wakimoto S, Okuyama R, Abe M, Kurikawa N, Kawamura S, Yamato M, Osumi J.

Abstract: A series of structurally novel stearoyl-CoA desaturase-1 (SCD-1) inhibitors has been identified by optimizing a hit from our corporate library. Preliminary structure-activity relationship (SAR) studies led to the discovery of the highly potent and orally bioavailable thiazole-based SCD-1 inhibitor, 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide (23a).

CiteXplore: 19540759

DOI: 10.1016/j.bmcl.2009.05.119