Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold

Microwave-assisted synthesis of potent PDE7 inhibitors containing a thienopyrimidin-4-amine scaffold

A series of novel thienopyrimidin-4-amines have been synthesized and evaluated as phosphodiesterase (PDE) inhibitors. A rationale for the observed selectivity against PDE7 has been obtained from molecular modelling studies on the most active compounds.

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Veröffentlicht in:Organic & biomolecular chemistry 2014-06, Vol.12 (24), p.4233-4242
Hauptverfasser: Sánchez, Ana I, Meneses, Ricardo, Mínguez, José M, Núñez, Araceli, Castillo, Rafael R, Filace, Fabiana, Burgos, Carolina, Vaquero, Juan J, Álvarez-Builla, Julio, Cortés-Cabrera, Alvaro, Gago, Federico, Terricabras, Emma, Segarra, Víctor
Format: Artikel
Sprache:eng
Schlagworte:
Binding Sites
Chemistry, Organic - methods
Cyclic Nucleotide Phosphodiesterases, Type 7 - antagonists & inhibitors
Cyclic Nucleotide Phosphodiesterases, Type 7 - chemistry
Hydrochloric Acid - chemistry
Inhibitory Concentration 50
Microwaves
Models, Molecular
Phosphodiesterase Inhibitors - chemical synthesis
Phosphodiesterase Inhibitors - chemistry
Phosphodiesterase Inhibitors - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Structure-Activity Relationship
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Beschreibung
Zusammenfassung:A series of novel thienopyrimidin-4-amines have been synthesized and evaluated as phosphodiesterase (PDE) inhibitors. A rationale for the observed selectivity against PDE7 has been obtained from molecular modelling studies on the most active compounds.
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob00175c