Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1′-{6-[5-(pyridin-3-ylmethyl)-1, 3, 4-oxadiazol-2-yl] pyridazin-3-yl}-3, 4-dihydrospiro [ …

…, M Konishi, T Takagi, S Wakimoto, J Ohsumi

文献索引：Uto, Yoshikazu; Ueno, Yuko; Kiyotsuka, Yohei; Miyazawa, Yuriko; Kurata, Hitoshi; Ogata, Tsuneaki; Yamada, Makiko; Deguchi, Tsuneo; Konishi, Masahiro; Takagi, Toshiyuki; Wakimoto, Satoko; Ohsumi, Jun European Journal of Medicinal Chemistry, 2010 , vol. 45, # 11 p. 4788 - 4796

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被引用次数: 23

摘要

In continuation of our investigation on novel stearoyl-CoA desaturase (SCD) 1 inhibitors, we have already reported on the structural modification of the benzoylpiperidines that led to a series of novel and highly potent spiropiperidine-based SCD1 inhibitors. In this report, we would like to extend the scope of our previous investigation and disclose details of the synthesis, SAR, ADME, PK, and pharmacological evaluation of the spiropiperidines with ...