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.
Departamento de Química Orgánica, Universidad de Alcalá, E-28871 Alcalá de Henares, Madrid, Spain. julio.alvarez.@uah.es.
Ana I
AI
Sánchez
Ricardo
R
Meneses
José M
JM
Mínguez
Araceli
A
Núñez
Rafael R
RR
Castillo
Fabiana
F
Filace
Carolina
C
Burgos
Juan J
JJ
Vaquero
Julio
J
Álvarez-Builla
Alvaro
A
Cortés-Cabrera
Federico
F
Gago
Emma
E
Terricabras
Víctor
V
Segarra
D001665:Binding Sites; D002625:Chemistry, Organic / Q000379:methods*; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006851:Hydrochloric Acid / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008872:Microwaves; D008958:Models, Molecular; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D010726:Phosphodiesterase Inhibitors; D011743:Pyrimidines; C476003:thienopyrimidine; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7; D006851:Hydrochloric Acid