Indolylpiperidine derivatives as potent and selective α1B adrenoceptor antagonists.
Basic Information
ID: ALA3608249
Journal: Bioorg Med Chem Lett
Title: Indolylpiperidine derivatives as potent and selective α1B adrenoceptor antagonists.
Authors: Hayashi R, Ohmori E, Moriwaki M, Kumagai H, Isogaya M.
Abstract: A series of novel indolylpiperidine derivatives were synthesized, and their pharmacological profiles were assessed at rat α1A and α1B adrenoceptors through in vitro binding studies. Compound 12 (2-(3-(4-(6-fluoro-1H-indol-3-yl)piperidin-1-yl)propyl)-1,2,3,4-tetrahydroisoquinoline) was a potent α1B adrenoceptor antagonist (Ki=0.61 nM) and was about 40-fold more selective for the α1B adrenoceptor than for the α1A adrenoceptor. In addition, useful structure-activity relationship information was acquired for further improving selectivity for the α1B adrenoceptor.
CiteXplore: 26238322
DOI: 10.1016/j.bmcl.2015.07.046
Patent ID: ┄