Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists

We describe novel alkylsulfones as potent CCR2 antagonists with reduced hERG channel activity and improved pharmacokinetics over our previously described antagonists. Several of these new alkylsulfones have a profile that includes functional antagonism of CCR2, in vitro microsomal stability, and ora...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Cherney, Robert J., Mo, Ruowei, Yang, Michael G., Xiao, Zili, Zhao, Qihong, Mandlekar, Sandhya, Cvijic, Mary Ellen, Charo, Israel F., Barrish, Joel C., Decicco, Carl P., Carter, Percy H.
Formato: Artigo
Idioma:Inglês
Publicado em: 2014
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4539253/
https://ncbi.nlm.nih.gov/pubmed/24613378
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2014.02.013
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