Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype

This Letter describes the synthesis and structure activity relationship (SAR) studies of structurally novel M(4) antagonists, based on a 4,6-disubstituted core, identified from a high-throughput screening campaign. A multi-dimensional optimization effort enhanced potency at both human and rat M(4) (...

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Publicado no:Bioorg Med Chem Lett
Main Authors: Bender, Aaron M., Weiner, Rebecca L., Luscombe, Vincent B., Cho, Hyekyung P., 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/PMC5508519/
https://ncbi.nlm.nih.gov/pubmed/28427812
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.04.009
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