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.
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.
4-(2-[2-(2(R)-Methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention
Cowart, Marlon,Faghih, Ramin,Curtis, Michael P.,Gfesser, Gregory A.,Bennani, Youssef L.,Black, Lawrence A.,Pan, Liping,Marsh, Kennan C.,Sullivan, James P.,Esbenshade, Timothy A.,Fox, Gerard B.,Hancock, Arthur A.
, p. 38 - 55 (2007/10/03)
H3 receptor antagonists based on a 2-aminoethylbenzofuran skeleton have been discovered, which are potent in vitro at human and rat H 3 receptors, with Ki values of 0.1-5.8 nM. Analogues were discovered with potent (0.01-1 mg/kg) cognition and attention enhancing properties in animal models. One compound in particular, 4-(2-[2-(2(R)- methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile (ABT-239), combined potent and selective H3 receptor antagonism and excellent pharmacokinetic and metabolic properties across species, with full efficacy in two behavioral models: a five-trial inhibitory avoidance acquisition model in rat pups at 0.1 mg/kg and a social recognition memory model in adult rats at 0.01 mg/kg. Furthermore, this compound did not stimulate locomotor activity and showed high selectivity for the induction of behavioral efficacy versus central nervous system based side effects. The potency and selectivity of this compound and of analogues from this class support the potential of H3 receptor antagonists for the treatment of cognitive dysfunction.