2. Academic Validation
  3. 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

  • Bioorg Med Chem Lett. 2008 Jun 1;18(11):3163-7. doi: 10.1016/j.bmcl.2008.04.071.
Subharekha Raghavan 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. subha_raghavan@merck.com
PMID: 18477506 DOI: 10.1016/j.bmcl.2008.04.071
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.

Figures