85084-36-2Relevant academic research and scientific papers
Amide-Oximes et hydroximates benzodioxaniques: synthese de nouveaux composes et etude en neuropsycho-pharmacologie
Davrinche, C,Nguyen-Tri-Xuong, E,Hamad, Y El,Reynaud, P,Rinjard, P,Tran, G
, p. 765 - 778 (1992)
Amide-oximes and benzodioxanic hydroximates: synthesis of new compounds and neuropsychopharmacological study.The authors describe the ON-(dialkylaminoalkyl) amide-oximes, benzodioxanic hydroximates and also the acetylated derivatives of the former compounds (I) which are detoxified.The hydroximates are obtained without structural ambiguity from thionoesters.Pharmacological testing via the main methods shows that some of these new compounds possess imipraminic, and others neuroleptic properties. benzodioxane/ amide-oxime / hydroximate / antidepressant / neuroleptic /
N-(Dialkylamino-2 ethyl) 2,3-dihydro 1,4-benzodioxin 2-carboximidamides-2: Synthesis and pharmacological activities
Davrinche,Nguyen-Tri-Xuong,Reynaud,Arnould-Guerin,Tran,Rinjard,Pieri
, p. 397 - 401 (2007/10/02)
In connection with the structure of piperoxan 1 and the recently described pharmacological properties of N-(diethylamino-2 ethyl) 2,3-dihydro 1,4-benzodioxin 2-carboximidamide 2a (R = C2H5, R' = H) and of idazoxan 3, different structural analogues have been prepared. These derivatives showed marked antiarrhythmic properties leading to the disappearance of extrasystoles and to a persistent regularization of the cardiac rhythm of rabbits perfused with aconitine. In addition, sedative effects have been detected using classical tests.
α-Adrenoreceptor reagents. I. Synthesis of some 1,4-benzodioxans as selective presynaptic α2-adrenoreceptor antagonists and potential antidepressants
Chapleo,Myers,Butler,Doxey,Roach,Smith
, p. 823 - 831 (2007/10/02)
The rational design of RX 781094, 2-(1,4-benzodioxan-2-yl)-2-imidazoline hydrochloride (5), a new potent and selective antagonist of α2-adrenoreceptors, is discussed. A compound that acts as an antagonist at presynaptic α2-adrenoreceptors could be an effective and novel treatment of depression because of its ability to increase the concentration of norepinephrine at central receptor sites. The effects of substituents in the aromatic and imidazoline rings have been examined, as well as the replacement of the imidazoline ring by an amidine function or by other heterocyclic ring systems. None of these derivatives are as potent or selective as 5, although some do display a degree of selectivity as antagonists. Some derivatives were found to possess agonist properties that, with the exception of 23, favored the postsynaptic site. Compounds 9, 12, 16, 21, 30, and 51 possessing presynaptic α2-adrenoreceptor antagonist and postsynaptic α1-adrenoreceptor partial agonist properties were also obtained, and these derivatives could be considered as potential antimigraine agents.
