Name of the group: “Synthesis and Isolation of Bioactive Compounds”

Our research group was founded in 1992 with the incorporation to the University of Valencia of the Professor Diego Cortes, coming from the Universities of Paris XI and Rouen (France) and the Professor Ernesto Estornell, coming from the University of Bologna (Italy), where they had developed research activity in the field of the structural chemistry of molecules with therapeutic interest and in the study of the mitochondrial complex I, respectively. The researches conducted by our group have been financed by several projects from the “Ministerio de Ciencia y Tecnología”, the “Consellería Valenciana de Cultura” and Pharmaceutical companies.

Since then, we are developing the chemical study, action mechanism and structure-activity relationships of both natural and synthetic compounds which are specific inhibitors of the complex I of the mitochondrial respiratory chain. "Acetogenins" are the sort of molecules that have turned out to be the more interesting into this field. They derive from poliacetates, and are biosynthesized in seeds of tropical species of the Annonaceae family. Their structure comprises an unsaturated lactone linked to a long hydrocarbonated chain interrupted by tetrahydrofuranic rings and usually by other oxygenated functions. Some of these molecules have become the most potent specific inhibitors in the mitochondrial complex I. The inhibition of this complex is implied in neurodegenerative illnesses such as the Parkinson’s disease.

On the other hand, we have developed a program for the synthesis of molecules with affinity for dopamine receptors, which can be used as neuroleptics and antiparkinsonians. In this sense, the design of synthesized molecules has been based on studies of molecular modelling carried out by the group of the Prof. Enriz of the National University of San Luis (Argentine). The synthesis of molecules with isoquinoline skeletons and indenopirida compounds has led to a significant specific affinity for any of the dopamine receptors. Recently, in vivo behavioral tests performed on one of the synthesized isoquinoline has allowed us to conclude that there is a new D₂ agonist with antidepressant activity.