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Repurposing human PDE4 inhibitors for neglected tropical diseases: Design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

A medicinal chemistry exploration of the human phosphodiesterase 4 (hPDE4) inhibitor cilomilast (1) was undertaken in order to identify inhibitors of phosphodiesterase B1 of Trypanosoma brucei (TbrPDEB1). T. brucei is the parasite which causes African sleeping sickness, a neglected tropical disease...

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Detalhes bibliográficos
Main Authors: Amata, Emanuele, Bland, Nicholas D., Hoyt, Charles T., Settimo, Luca, Campbell, Robert K., Pollastri, Michael P.
Formato: Artigo
Idioma:Inglês
Publicado em: 2014
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4155488/
https://ncbi.nlm.nih.gov/pubmed/25127163
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2014.07.063
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