Author/Authors :
Subharekha Raghavan، نويسنده , , G. Scott Tria، نويسنده , , Hong C. Shen، نويسنده , , Fa-Xiang Ding، نويسنده , , Andrew K. Taggart، نويسنده , , Ning Ren، نويسنده , , Larrisa C. Wilsie، نويسنده , , Mihajlo L. Krsmanovic، نويسنده , , Tom G. Holt، نويسنده , , Michael S. Wolff، نويسنده , , M. Gerard Waters، نويسنده , , Milton L. Hammond، نويسنده , , James R. Tata، نويسنده , , Steven L. Colletti، نويسنده ,
Abstract :
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.
