2. Academic Validation
  3. Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors

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

  • J Med Chem. 2014 Oct 23;57(20):8590-607. doi: 10.1021/jm501090m.
Ana M García 1,  José Brea,  Jose A Morales-García,  Daniel I Perez,  Alejandro González,  Sandra Alonso-Gil,  Irene Gracia-Rubio,  Clara Ros-Simó,  Santiago Conde,  María Isabel Cadavid,  María Isabel Loza,  Ana Perez-Castillo,  Olga Valverde,  Ana Martinez,  Carmen Gil
Affiliations

Affiliation

  • 1 Centro de Investigaciones Biológicas (CSIC) , Ramiro de Maeztu 9, 28040 Madrid, Spain.
PMID: 25264825 DOI: 10.1021/jm501090m
Abstract

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.

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