Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists

This Letter describes the synthesis and structure activity relationship (SAR) studies of structurally novel M(4) antagonists, based on a 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazine core, identified from a high-throughput screening campaign. A multidimensional optimizati...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Bender, Aaron M., Weiner, Rebecca L., Luscombe, Vincent B., Ajmera, Sonia, Cho, Hyekyung P., Chang, Sichen, Zhan, Xiaoyan, Niswender, Colleen M., Engers, Darren W., Bridges, Thomas M., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6659418/
https://ncbi.nlm.nih.gov/pubmed/28633897
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.05.042
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