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Discovery of Diaryl Ether Substituted Tetrahydrophthalazinones as TbrPDEB1 Inhibitors Following Structure-Based Virtual Screening

Several members of the 3′,5′-cyclic nucleotide phosphodiesterase (PDE) family play an essential role in cellular processes, which has labeled them as interesting targets for various diseases. The parasitic protozoan Trypanosoma brucei, causative agent of human African trypanosomiasis, contains sever...

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Principais autores: Erik de Heuvel, Albert J. Kooistra, Ewald Edink, Sjors van Klaveren, Jeffrey Stuijt, Tiffany van der Meer, Payman Sadek, Dorien Mabille, Guy Caljon, Louis Maes, Marco Siderius, Iwan J. P. de Esch, Geert Jan Sterk, Rob Leurs
Formato: Artigo
Idioma:Inglês
Publicado em: Frontiers Media S.A. 2021-01-01
coleção:Frontiers in Chemistry
Assuntos:
virtual screening
phosphodiesterase TbrPDEB1
trypanosomiasis
cAMP
tetrahydrophthalazinones
medicinal chemistry
Acesso em linha:https://www.frontiersin.org/articles/10.3389/fchem.2020.608030/full
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