名称:
                                2,4-Diaminopyridine δ-opioid receptor agonists and their associated hERG pharmacology
                             
                            
                                摘要:
                                A number of libraries were produced to explore the potential of 2,4-diaminopyridine lead 1. The resulting diaminopyridines proved to be potent and selective delta-opioid receptor agonists. Several rounds of lead optimisation using library chemistry identified compound 17 which went on to show efficacy in an electromyography model of neuropathic pain. The structure-activity relationship of the series against the hERG ion channel proved to be a key selectivity hurdle for the series. (C) 2009 Elsevier Ltd. All rights reserved.
                             
                                                            
                                    DOI:
                                    10.1016/j.bmcl.2009.01.106