Studies towards topical selective β 2-adrenoceptor agonists with a long duration of action

β 2-Adrenoceptor agonists with basic and acidic groups R were prepared and investigated in vitro and in vivo. β 2-Adrenoceptor agonists with basic and acidic groups attached via an alkyl linker to the phenyl ethanolamine core were prepared and investigated in vitro and in vivo. The compounds exhibit...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 19; no. 17; pp. 5237 - 5240
Main Authors Bouyssou, Thierry, Rudolf, Klaus, Hoenke, Christoph, Lustenberger, Philipp, Schnapp, Andreas, Konetzki, Ingo
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2009
Subjects
Adrenoceptor agonists
Asthma
Benzoxazinone
Beta2
COPD
Duration of action
Benzoxazinone
Beta2
Adrenoceptor agonists
Duration of action
Asthma
COPD
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Summary:β 2-Adrenoceptor agonists with basic and acidic groups R were prepared and investigated in vitro and in vivo. β 2-Adrenoceptor agonists with basic and acidic groups attached via an alkyl linker to the phenyl ethanolamine core were prepared and investigated in vitro and in vivo. The compounds exhibited a high potency in a functional cellular assay and a bronchoprotective effect in a guinea pig model which lasted over the complete study period of 5 h.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.06.104