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| Título: | Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors |
Autor: | García, Ana M. CSIC ORCID; Brea, José Manuel; Morales-García, José A. CSIC ORCID; Pérez, Daniel I. CSIC ORCID; González, Alejandro CSIC ORCID; Alonso-Gil, Sandra CSIC; Conde, Santiago CSIC; Cadavid, María Isabel; Loza, María Isabel; Pérez Castillo, Ana CSIC ORCID; Martínez Gil, Ana CSIC ORCID ; Gil, Carmen CSIC ORCID | Fecha de publicación: | 2014 | Editor: | American Chemical Society | Citación: | Journal of Medicinal Chemistry 57(20): 8590-8607 (2014) | Resumen: | A 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 | DOI: | 10.1021/jm501090m | Identificadores: | doi: 10.1021/jm501090m issn: 0022-2623 e-issn: 1520-4804 |
| Aparece en las colecciones: | (CIB) Artículos (IQM) Artículos (IIBM) Artículos |
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