Acidic elements in histamine H(3) receptor antagonists.
Article Details
- CitationCopy to clipboard
Sander K, von Coburg Y, Camelin JC, Ligneau X, Rau O, Schubert-Zsilavecz M, Schwartz JC, Stark H
Acidic elements in histamine H(3) receptor antagonists.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1581-4. doi: 10.1016/j.bmcl.2010.01.089. Epub 2010 Jan 21.
- PubMed ID
- 20138762 [ View in PubMed]
- Abstract
Antagonists of the human histamine H(3) receptor (hH(3)R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK(a) values to figure out that the hH(3)R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH(3)R affinities in the nanomolar concentration range. Additionally, selected ligands were tested but failed as dual acting hH(3)R/hPPAR (human peroxisome proliferator-activated receptor) ligands.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha EC 50 (nM) >10000 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 30 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 100 N/A N/A Details