Potent and selective α1A adrenoceptor partial agonists—Novel imidazole frameworks
摘要:
Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity. (C) 2009 Elsevier Ltd. All rights reserved.
For the purpose of providing a GSK-3β inhibitor containing a 2-aminopyridine compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3β-related pathology or disease, the present invention provides a GSK-3β inhibitor containing a compound represented by the formula (IA):
wherein each symbol is as defined in the specification.
or a salt thereof or a prodrug thereof.
Potent and selective α1A adrenoceptor partial agonists—Novel imidazole frameworks
作者:Gavin A. Whitlock、Paul E. Brennan、Lee R. Roberts、Alan Stobie
DOI:10.1016/j.bmcl.2009.03.162
日期:2009.6
Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity. (C) 2009 Elsevier Ltd. All rights reserved.