460747-73-3Relevant articles and documents
Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents
Bao, Xiaofeng,Jin, Yanyan,Liu, Xiaolu,Liao, Hong,Zhang, Luyong,Pang, Tao
, p. 6761 - 6775 (2014/02/14)
A novel class of H3 receptor antagonists, XB-1 analogues based on benzophenone or oxydibenzene scaffolds were synthesized, and their biological activities were evaluated to determine their in vitro neuroprotective effects against Aβ25-35-induced damage in primary cortical neurons and against glutamate-induced neuronal injury in primary cerebellar granule neurons. The results indicated that all of the tested analogues displayed neuroprotective activity at 0.1 μM or 1 μM. These findings may provide new insights into the development of novel promising H3 receptor antagonists with potential neuroprotective activity.
Synthesis and SAR of 5-amino- and 5-(aminomethyl)benzofuran histamine H3 receptor antagonists with improved potency
Sun, Minghua,Zhao, Chen,Gfesser, Gregory A.,Thiffault, Christine,Miller, Thomas R.,Marsh, Kennan,Wetter, Jill,Curtis, Michael,Faghih, Ramin,Esbenshade, Timothy A.,Hancock, Arthur A.,Cowart, Marlon
, p. 6482 - 6490 (2007/10/03)
A new series of H3 receptor antagonists was discovered with nanomolar and subnanomolar affinities at human and rat H3 receptors. Starting from an earlier, more structurally limited series of benzofurans, the present series of compounds demonstrated increased structural variety and flexibility with greater in vitro potency. One compound in particular, {2-[2-(2-(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl}(5-nitropyridin-2-yl) amine (7h), gave the best binding potency (human Ki of 0.05 nM, rat Ki of 0.11 nM), which represented a 9-fold (in human) and an 11-fold (in rat) improvement over ABT-239 (compound 5), a compound previously reported to have excellent in vitro potency and in vivo efficacy. The synthesis, SAR of the H3 binding affinities, in vitro assay for phospholipidosis, and pharmacokinetic properties of the new compounds are described.
Structure-activity relationships of arylbenzofuran H3 receptor antagonists
Gfesser, Gregory A.,Faghih, Ramin,Bennani, Youssef L.,Curtis, Michael P.,Esbenshade, Timothy A.,Hancock, Arthur A.,Cowart, Marlon D.
, p. 2559 - 2563 (2007/10/03)
An SAR study of histamine H3 receptor antagonists based on substituted (R)-2-methyl-1-[2-(5-phenyl-benzofuran-2-yl)-ethyl]-pyrrolidines is presented.