Title of article
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: Application to the discovery of potent niacin receptor agonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
3163
To page
3167
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.
Keywords
Niacin receptor agonists , Surrogate for anthranilic acid , Tetrahydro anthranilic acid
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799522
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