62812-22-0Relevant academic research and scientific papers
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as β2-adrenoceptor agonists
Hoenke, Christoph,Bouyssou, Thierry,Tautermann, Christofer S.,Rudolf, Klaus,Schnapp, Andreas,Konetzki, Ingo
scheme or table, p. 6640 - 6644 (2010/06/12)
Novel β2-agonists with a 5-hydroxy-4H-benzo[1,4]oxazin-3-one moiety as head group are described. Systematic chemical variations at the phenethylamine residue of these compounds lead to the discovery of compound 6m as potent, full agonist of the β2-adrenoceptor with a high β1/β2-selectivity. Molecular modeling revealed an interaction between the carboxylic acid group of 6m and a lysine residue (K305) of the β2-receptor as putative explanation for the high observed selectivity. Further, compound 6m displayed in a guinea pig in vivo model a complete reversal of acetylcholine induced bronchoconstriction which lasted over the complete study time of 5 h.
Trifluoromethyl substituted compounds having antidepressive activity
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, (2008/06/13)
A compound of the formula (I) and pharmaceutically acceptable acid addition salts thereof, in which formula the group R o is trifluoromethyl. Pharmaceutical compositions containing these compounds are useful for treatment of depressive disorders
