Anthranilic acid replacements in a niacin receptor agonist.
Article Details
- CitationCopy to clipboard
Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S
Anthranilic acid replacements in a niacin receptor agonist.
Bioorg Med Chem Lett. 2010 Jun 1;20(11):3426-30. doi: 10.1016/j.bmcl.2010.04.001. Epub 2010 Apr 8.
- PubMed ID
- 20444602 [ View in PubMed]
- Abstract
Niacin is an effective drug for raising HDL cholesterol. However, niacin must be taken in large doses and significant side effects are often observed, including facial flushing, loss of glucose tolerance, and liver toxicity. An anthranilic acid was identified as an agonist of the niacin receptor. In order to improve efficacy and provide structural diversity, replacements for the anthranilic acid were investigated and several compounds with improved properties were identified.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Niacin Hydroxycarboxylic acid receptor 2 EC 50 (nM) 1000 N/A N/A Details Niacin Hydroxycarboxylic acid receptor 2 IC 50 (nM) 140 N/A N/A Details