733783-33-0Relevant articles and documents
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists
Swanson, Devin M.,Shah, Chandra R.,Lord, Brian,Morton, Kirsten,Dvorak, Lisa K.,Mazur, Curt,Apodaca, Richard,Xiao, Wei,Boggs, Jamin D.,Feinstein, Mark,Wilson, Sandy J.,Barbier, Ann J.,Bonaventure, Pascal,Lovenberg, Timothy W.,Carruthers, Nicholas I.
experimental part, p. 4413 - 4425 (2009/12/24)
A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H3 receptor (hH3R). Nine of the twenty-eight compounds tested were found to possess a hH3R Ki of less than 5 nM and consisted of a diverse range of central hetero-aromatic linkers (pyridine, pyrazine, oxazole, isoxazole, thiazole, furan, thiophene, and pyrrole). One member of this series, (4-isopropyl-piperazin-1-yl)-(6-piperidin-1-ylmethyl-pyridin-3-yl)-methanone (37), was found to be a high affinity, selective antagonist that crosses the blood-brain barrier and occupies H3 receptors after oral administration in the rat.
