Pharmacochemistry Laboratory

 
 
  Subjets & Research Areas
 
Subjects & Research Areas
 

a) Synthesis of Isoquinolines and Indenopyridines with Dopaminergic Activity: we have prepared various families of "isoquinolines" by Bischler- Napieralsky cyclodehydration to generate the isoquinoline nucleus. Affinity studies of these molecules for dopamine receptors (D1-like and D2-like) have been carried out on rat brain synaptosomes. As a result of these studies, we have synthesized some D2-dopamine receptor agonists with antidepressant activity. Other skeletons are being synthesized to obtain the most therapeutically effective drugs, like "indenopyridines" compounds. Recently, we have synthesized a series of isoquinolines containing the nitrogen atom into a lactam ring, pyrrolo [2,1-a] isoquinolines-3-ones, which have shown antimicrobial activity against various pathogens.

 
1-Alquil-isoquinoleína dopaminergica
[Berenguer et al. Bioorganic & Medicinal Chemistry 2009 17, 4968-4980.
Andujar et al. Journal of Molecular Modeling. 2012, 18, 419–431.]
 

b) Antitumor Acetogenins and Natural Insecticides:For many years, our research group has studied these original ASM. Recently, growing interest has been shown in their important pharmacological activities, which has been acknowledged by many companies. These compounds are potent mitochondrial respiratory chain inhibitors of complex I (the nM range), and are abundant in the seeds of tropical fruits belonging to the Annonaceae family, including the custard apple and soursop (Annona cherimolia and A. muricata, respectively). The potential application of acetogenins as new antitumor agents and insecticides means that they are main focal point of numerous research studies worldwide.

 
Diacetil-guanacona (acetogenina)
[Barrachina et al. Bioorganic & Medicinal Chemistry 2007 15, 4369-4381.]
 

c) Industrial Research: Synthesis and Isolation of New Bioactive Molecules: In the last 15 years, our group has carried out several projects with pharmaceutical companies, among which the following stand out: Laboratories Servier, Merck Sharp & Dohme, Medina Foundation and Valentia Biopharma. In most cases, our contribution has consisted in obtaining natural and synthetic compounds that act against various biological targets. Some of the results obtained have led to some patents, doctoral theses or scientific publications in international journals. In other cases, confidentiality matters have meant that some results cannot be reported for the time being.

 
Benzoildihidroisoquinoleínas antitumorales
[Bermejo et al. Journal of Medicinal Chemistry 2002, 45, 5058-5068.]