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Título

Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors

Autor García, Ana M. ; Brea, José; Morales-García, José A. ; Pérez, Daniel I.; González, A. ; Alonso-Gil, Sandra ; Conde, Santiago ; Cadavid, María Isabel; Loza, María Isabel; Pérez Castillo, Ana ; Martínez, Ana ; Gil, Carmen
Fecha de publicación 2014
EditorAmerican Chemical Society
Citación Journal of Medicinal Chemistry 57(20): 8590-8607 (2014)
ResumenA forward chemical genetic approach was followed to discover new targets and lead compounds for Parkinson's disease (PD) treatment. By analysis of the cell protection produced by some small molecules, a diphenyl sulfide compound was revealed to be a new phosphodiesterase 7 (PDE7) inhibitor and identified as a new hit. This result allows us to confirm the utility of PDE7 inhibitors as a potential pharmacological treatment of PD. On the basis of these data, a diverse family of diphenyl sulfides has been developed and pharmacologically evaluated in the present work. Moreover, to gain insight into the safety of PDE7 inhibitors for human chronic treatment, we evaluated the new compounds in a surrogate emesis model, showing nonemetic effects.
Descripción et al.
URI http://hdl.handle.net/10261/114908
DOI10.1021/jm501090m
Identificadoresdoi: 10.1021/jm501090m
issn: 0022-2623
e-issn: 1520-4804
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