Synthesis and pharmacological evaluation of some WB4101 analogues bearing a naphthodioxanic nucleus.
Three WB4101 analogues, bearing a 1,4-naphthodioxanic system, were synthesized. The decrease of the alpha-blocking activity found for these compounds, showed that extension of the aromatic area in the dioxanic moiety of such benzodioxanic derivative, hinders the drug-receptor interaction.
D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis*; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003000:Clonidine / Q000494:pharmacology; D004146:Dioxanes / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004147:Dioxins / Q000494:pharmacology*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats; D013569:Synapses / Q000187:drug effects
D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D004147:Dioxins; C042678:2-((2-ethyl(2,6-dimethoxyphenoxy)amino)methyl)1,4-dioxane-(2,3-b)naphthalene; C042680:3-((-(2,6-dimethoxyphenoxy)ethyl)amino)methyl-1,4-dioxane(1,2-b)naphthalene; C042679:2-((2-(2,6-dimethoxyphenoxy)ethyl)amino)methyl-1,4-dioxane(1,2-b)naphthalene; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane; D003000:Clonidine; D009638:Norepinephrine