Design, synthesis, and structure–activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors

…, T Yamashita, A Kina, M Funata, A Mizukami…

文献索引：Kamata, Makoto; Yamashita, Tohru; Kina, Asato; Funata, Masaaki; Mizukami, Atsushi; Sasaki, Masako; Tani, Akiyoshi; Funami, Miyuki; Amano, Nobuyuki; Fukatsu, Kohji Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3643 - 3647

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被引用次数: 11

摘要

Spiro-lactone (S)-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor and was found to be metabolically liable in human hepatic microsomes. To remove one of the risk factors in human study by improving the metabolic stability, we focused on modifying the spiro-lactone ring and the benzothiophene portion of the molecule. Spiro-imide derivative 8c containing a 6-methylthieno [2, 3-b] pyridine core exhibited potent ACC inhibitory activity and favorable ...