Pharmacological tools based on imidazole scaffold proved the utility of PDE10A inhibitors for Parkinson's disease

Garcia, Ana M.; Salado, Irene G.; Perez, Daniel I.; Brea, Jose; Morales-Garcia, Jose A.; Gonzalez-Garcia, Alejandro; Cadavid, MariaIsabel; Isabel Loza, Maria; Javier Luque, Francisco; Perez-Castillo, Ana; Martinez, Ana; Gil, Carmen

Abstract

Since neuroinflammation is partially mediated by cAMP levels and PDE10A enzyme is able to regulate these levels being highly expressed in striatum, its inhibitors emerged as useful drugs to mitigate this inflammatory process and hence the neuronal death associated with Parkinson's disease (PD). Methodology results: To study the utility of PDE10A as a pharmacological target for PD, in this work we propose the search and development of new PDE10A inhibitors that could be useful as pharmacological tools in models of the disease and presumably as potential drug candidates. By using different medicinal chemistry approaches we have discovered imidazole-like PDE10A inhibitors and showed their neuroprotective actions. Conclusion: Here, we demonstrate the neuroprotective effect of PDE10A inhibitors in cellular models of PD.

Más información

Título según WOS: ID WOS:000402256200005 Not found in local WOS DB
Título de la Revista: FUTURE MEDICINAL CHEMISTRY
Volumen: 9
Número: 8
Editorial: FUTURE SCI LTD
Fecha de publicación: 2017
Página de inicio: 731
Página final: 748
DOI:

10.4155/fmc-2017-0005

Notas: ISI