| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363346 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Antagonists of the human histamine H3 receptor (hH3R) 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 pKa values to figure out that the hH3R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH3R affinities in the nanomolar concentration range. Additionally, selected ligands were tested but failed as dual acting hH3R/hPPAR (human peroxisome proliferator-activated receptor) ligands.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kerstin Sander, Yvonne von Coburg, Jean-Claude Camelin, Xavier Ligneau, Oliver Rau, Manfred Schubert-Zsilavecz, Jean-Charles Schwartz, Holger Stark,