- Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Bioorganic & medicinal chemistry letters (2008-05-15)
Subharekha Raghavan, G Scott Tria, Hong C Shen, Fa-Xiang Ding, Andrew K Taggart, Ning Ren, Larrisa C Wilsie, Mihajlo L Krsmanovic, Tom G Holt, Michael S Wolff, M Gerard Waters, Milton L Hammond, James R Tata, Steven L Colletti
PMID18477506
摘要
The design, synthesis, and biological activity of a series of cycloalkene acid-based niacin receptor agonists are described. This led to the discovery that tetrahydro anthranilic acid is an excellent surrogate for anthranilic acid. Several compounds were identified that were potent against the niacin receptor, had enhanced cytochrome P450 selectivity against subtypes CYP2C8 and CYP2C9, and improved oral exposure in mice.
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烟酸, BioReagent, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥98%