Design and synthesis of pyridazinone-based 5-HT sub(2C) agonists

The SAR of a series of pyridazinone derived 5-HT sub(2C) agonists has been explored and resulted in identification of a compound with excellent levels of 5-HT sub(2C) functional agonism and selectivity over 5- HT sub(2A) and 5-HT sub(2B). This compound displayed good in vivo efficacy in pre-clinical...

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Published inBioorganic & medicinal chemistry letters Vol. 19; no. 19; pp. 5791 - 5795
Main Authors Allerton, Charlotte MN, Andrews, Mark D, Blagg, Julian, Ellis, David, Evrard, Edel, Green, Martin P, Liu, Kevin K-C, McMurray, Gordon, Ralph, Michael, Sanderson, Vivienne, Ward, Robin, Watson, Lesa
Format Journal Article
LanguageEnglish
Published 01.10.2009
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Summary:The SAR of a series of pyridazinone derived 5-HT sub(2C) agonists has been explored and resulted in identification of a compound with excellent levels of 5-HT sub(2C) functional agonism and selectivity over 5- HT sub(2A) and 5-HT sub(2B). This compound displayed good in vivo efficacy in pre-clinical models of stress urinary incontinence, despite having physiochemical properties commensurate with impaired CNS penetration.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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ObjectType-Feature-1
ISSN:0960-894X
DOI:10.1016/j.bmcl.2009.07.136