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

…, J Álvarez-Builla, A Cortés-Cabrera, F Gago…

Index: Sanchez, Ana I.; Meneses, Ricardo; Minguez, Jose M.; Nunez, Araceli; Castillo, Rafael R.; Filace, Fabiana; Burgos, Carolina; Vaquero, Juan J.; Alvarez-Builla, Julio; Cortes-Cabrera, Alvaro; Gago, Federico; Terricabras, Emma; Segarra, Victor Organic and Biomolecular Chemistry, 2014 , vol. 12, # 24 p. 4233 - 4242

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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. ... On the other hand, in the structure of the dual-specific PDE1B, the key histidine residue has been suggested to enable the invariant glutamine to toggle depending on whether it binds cAMP or cGMP.

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