126395-05-9Relevant academic research and scientific papers
Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors
García, Ana M.,Brea, José,Morales-García, Jose A.,Perez, Daniel I.,González, Alejandro,Alonso-Gil, Sandra,Gracia-Rubio, Irene,Ros-Simó, Clara,Conde, Santiago,Cadavid, María Isabel,Loza, María Isabel,Perez-Castillo, Ana,Valverde, Olga,Martinez, Ana,Gil, Carmen
, p. 8590 - 8607 (2014/12/11)
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.
Diaryl sulfide-based inhibitors of trypanothione reductase: Inhibition potency, revised binding mode and antiprotozoal activities
Stump, Bernhard,Eberle, Christian,Kaiser, Marcel,Brun, Reto,Krauth-Siegel, R. Luise,Diederich, Francois
supporting information; experimental part, p. 3935 - 3947 (2009/06/28)
Trypanothione reductase (TR) is an essential enzyme of trypanosomatids and therefore a promising target for the development of new drugs against African sleeping sickness and Chagas′ disease. Diaryl sulfides with a central anilino moiety, decorated with a
