Discovery Of Potent Alpha 1l-Adrenoceptor Agonists: Design And Synthesis Of Bicyclic Derivatives
Bioorganic & Medicinal Chemistry Letters（2015）
Abstract
We aimed to create a novel and potent α1L-adrenoceptor agonist because such agonists are possible drug candidates for stress urinary incontinence. We used ligand-based drug design and evaluated the α1L-adrenoceptor agonist activity of the designed compounds. Among them, tetrahydroquinoline derivative 50 showed the most potent activity (ratio of noradrenaline half maximal effective concentration, 0.0028) and effectively induced contraction of rat bladder neck.
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