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Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors
Authors:Ana I Sánchez  Valentín Martínez-Barrasa  Carolina Burgos  Juan J Vaquero  Julio Alvarez-Builla  Emma Terricabras  Víctor Segarra
Institution:1. Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain;2. Almirall-Prodesfarma, Laureà Miró, 408-410, 08980 Sant Felíu de Llobregat, Barcelona, Spain
Abstract:The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7.
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