2013, Publicación

Sánchez et al. Bioorg. Med. Chem.. 2013;21(8):2370 -2378. Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.

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Bioorg. Med. Chem. 2013; 21(8):2370 -2378. doi: 10.1016/j.bmc.2013.01.067

Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.

A.I. Sánchez1, V. Martínez-Barrasa2, C. Burgos3, J.J. Vaquero4, J. Alvarez-Builla, E. Terricabras, V. Segarra

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.  3. Centro Nacional de Referencia Sobre Contaminantes Orgánicos Persistentes (CNRCOP), Parque Científico Tecnológico, Universidad de Alcalá, C/Punto Net, 4, 28871 Alcalá de Henares, Madrid, Spain.  4. Pharma Mar S.A., Avda. De los Reyes, 1 Pol. Ind. La Mina-Norte, 28770 Colmenar Viejo, Madrid, Spain.

Resumen

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. © 2013 Elsevier Ltd. All rights reserved.

graphical abstract