2-(4,5-Dihydroimidazol-2-yl)benzimidazoles as highly selective imidazoline I2/adrenergic α2 receptor ligands
2-(4,5-Dihydroimidazol-2-yl)benzimidazoles have been identified as selective imidazoline I2/α2-adrenoceptor ligands. 4-Methyl (2) and 4-chloro (4) derivatives display I2 affinity at nanomolar concentration (Ki = 4.4 and 17.7 nM, respectively) and high I2/α2 selectivity ratio = 4226 and 5649, respectively. An evidence has been obtained that pKa value influences considerably the I2/α2-selectivity ratio of this class of imidazoline I2 receptor ligands.
Saczewski, Francieszek,Tabin, Piotr,Tyacke, Robin J.,Maconie, Alys,Saczewski, Jaroslaw,Kornicka, Anita,Nutt, David J.,Hudson, Alan L.
p. 6679 - 6685
(2007/10/03)
Synthesis of substituted aryl amidines from aminoacetonitriles
Aryl aminoacetonitriles are oxidized by NiO2-H2O or MnO2 in the presence of a wide range of NH2-containing compounds to afford aryl amidines, presumably via iminium intermediates. A 'one-pot' procedure for the preparation of heteroaryl amidines from N-containing heteroaryl halides through a process comprising sequential SNAr substitution and oxidation has also been developed.
Yin, Zhiwei,Zhang, Zhongxing,Zhu, Juliang,Wong, Henry,Kadow, John F.,Meanwell, Nicholas A.,Wang, Tao
p. 4919 - 4923
(2007/10/03)
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