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

Ana I. Sánchez; Ricardo Meneses; José M. Mínguez; Araceli Núñez; Rafael R. Castillo; Fabiana Filace; Carolina Burgos; Juan J. Vaquero; Julio Álvarez-Builla; Alvaro Cortés-Cabrera; Federico Gago; Emma Terricabras; Víctor Segarra

doi:10.1039/C4OB00175C

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

Ana I. Sánchez,*^a Ricardo Meneses,^a José M. Mínguez,^a Araceli Núñez,^a Rafael R. Castillo,^a Fabiana Filace,^a Carolina Burgos,^a Juan J. Vaquero,^a Julio Álvarez-Builla,*^a Alvaro Cortés-Cabrera,^b Federico Gago,^b Emma Terricabras^c and Víctor Segarra^c

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^a Departamento de Química Orgánica, Universidad de Alcalá, E-28871 Alcalá de Henares, Madrid, Spain
E-mail: julio.alvarez.@uah.es
Tel: +34 918 854 680

^b Departamento de Ciencias Biomédicas, Universidad de Alcalá, E-28871 Alcalá de Henares, Madrid, Spain
Tel: +34 918 854 514

^c Almirall-Prodesfarma, Laureà Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain

Abstract

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.

Organic & Biomolecular Chemistry

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

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

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