Sander, Kerstin et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2010 |CAS: 86393-32-0

The Article related to h3 antagonist acidic moiety preparation structure activity crystal structure, antihistamine h3 antagonist acidic moiety preparation structure activity, Pharmacology: Structure-Activity and other aspects.Application of 86393-32-0

On March 1, 2010, Sander, Kerstin; von Coburg, Yvonne; Camelin, Jean-Claude; Ligneau, Xavier; Rau, Oliver; Schubert-Zsilavecz, Manfred; Schwartz, Jean-Charles; Stark, Holger published an article.Application of 86393-32-0 The title of the article was Acidic elements in histamine H3 receptor antagonists. And the article contained the following:

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 pK a 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. Addnl., selected ligands were tested but failed as dual acting hH3R/hPPAR (human peroxisome proliferator-activated receptor) ligands. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application of 86393-32-0

The Article related to h3 antagonist acidic moiety preparation structure activity crystal structure, antihistamine h3 antagonist acidic moiety preparation structure activity, Pharmacology: Structure-Activity and other aspects.Application of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics