| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374050 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
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 pharmacokinetic profiles in rats.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Makoto Kamata, Tohru Yamashita, Asato Kina, Masaaki Funata, Atsushi Mizukami, Masako Sasaki, Akiyoshi Tani, Miyuki Funami, Nobuyuki Amano, Kohji Fukatsu,