title: Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.
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.
authors: Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain.
authors: Ana I
authors: AI
authors: Sánchez
authors: Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain.
authors: Valentín
authors: V
authors: Martínez-Barrasa
authors: Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain. Electronic address: carolina.burgos@uah.es.
authors: Carolina
authors: C
authors: Burgos
authors: Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain.
authors: Juan J
authors: JJ
authors: Vaquero
authors: Departamento de Quimica Orgánica, Universidad de Alcala, 28871 Alcalá de Henares, Madrid, Spain.
authors: Julio
authors: J
authors: Alvarez-Builla
authors: Almirall-Prodesfarma, Laureà Miró, 408-410, 08980 Sant Felíu de Llobregat, Barcelona, Spain.
authors: Emma
authors: E
authors: Terricabras
authors: Almirall-Prodesfarma, Laureà Miró, 408-410, 08980 Sant Felíu de Llobregat, Barcelona, Spain.
authors: Víctor
authors: V
authors: Segarra
mesh_terms: D054708:Cyclic Nucleotide Phosphodiesterases, Type 7 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D010726:Phosphodiesterase Inhibitors; D011799:Quinazolines; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7