309728-75-4Relevant academic research and scientific papers
Synthesis and β-blocking activity of (R,S)-(E)-oximeethers of 2,3-dihydro-1,8-naphthyridine and 2,3-dihydrothiopyrano[2,3-b]pyridine: Potential antihypertensive agents - Part IX
Ferrarini, Pier Luigi,Mori, Claudio,Badawneh, Muwaffag,Calderone, Vincenzo,Greco, Rosamiria,Manera, Clementina,Martinelli, Adriano,Nieri, Paola,Saccomanni, Giuseppe
, p. 815 - 826 (2007/10/03)
The synthesis of oximeethers of 2,3-dihydro-1,8-naphthyridine and 2,3-dihydrothiopyrano[2,3-b]pyridine is described. These compounds exhibit a selective β-blocking activity, with a selectivity towards β2-receptors. Groups in the N1 position giving rise to a considerable steric hindrance led to a higher β2-blocking selectivity, whereas groups creating a moderate hindrance caused a weak but significant decrease in β2-antagonist potency. Substitution of the N1-R group with a sulfur atom led to compounds possessing β1-, β2- and β3-blocking properties. Compounds 9c1 and 10a1 showed a β3-antagonist activity slightly lower than that of propranolol. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
