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

…, Y Miyazawa, H Kurata, T Deguchi, N Watanabe…

文献索引：Uto, Yoshikazu; Ogata, Tsuneaki; Harada, Jun; Kiyotsuka, Yohei; Ueno, Yuko; Miyazawa, Yuriko; Kurata, Hitoshi; Deguchi, Tsuneo; Watanabe, Nobuaki; Takagi, Toshiyuki; Wakimoto, Satoko; Okuyama, Ryo; Abe, Manabu; Kurikawa, Nobuya; Kawamura, Sayako; Yamato, Michiko; Osumi, Jun Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4151 - 4158

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被引用次数: 18

摘要

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).