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Research Programmes

Chemistry & Molecular Pharmacology

Bioactive peptidomimetic and heterocycles (Biosyner)

mrubiralta

Màrius Rubiralta

Principal Investigator
Professor (Pharmacology and Medicinal Chemistry Dept. - UB)

Office Tel : +34 93 403 71 04
Lab Tel : +34 93 403 71 08
e-mail : marius.rubiraltairbbarcelona.org

Background

The drug discovery process relies on the preparation of the key bioactive compounds in pure form. Therefore, synthetic and analytical technologies are critical for the development of this kind of projects. Exploration in new reactivity pathways dealing with heterocycles (structures frequently found in drugs), new types of peptide-like molecules and the efficient separation of enantiomers constitute methodological tools in the first steps of drug discovery.

Research Interests

Our main objective is to obtain new use ful molecules to be applied in the biomedical field. To this end, our approach is based on heterocyclic and peptide synthesis. Our main therapeutic targets are cancer, AIDS, and infectious processes.

We also study chiral molecules as a tool in the separation of enantiomers by several chromatography-related technologies.

We focus on the development of new synthetic pathways for rapid and efficient synthesis of heterocyclic systems. In this respect, we explore new multi-component reactions with nitrogen and oxygen heterocycles.

Research Lines

Conformationally constrained peptidomimetics
We select known peptides of structural and bioactive interest to be used as models, and we synthesize small libraries of constrained derivatives designed by pharmacomodulation. Once purified and fully characterized, the new molecules are submitted to SAR studies in order to improve the lead compounds.

Enantioselective molecular recognition
The main objective is to study the enantioselective recognition mechanism and its application to the separation of enantiomers, both at the analytic and the preparative level. A knowledge of this mechanism will lead to the design of new chiral selectors with a wide range of applications, or selectors especially adapted to the separation of certain families of compounds. The study involves the use of low molecular weight chiral selectors (derived from enantiomerically pure alfa-amino acids) and chiral macromolecules (derived from polysaccharides). We examine the application of all of these in analytical separation techniques (HPLC or CE), and their use as selectors in other preparative chromatographic-related techniques. Particular effort is devoted to the separation of enantiomers through enantioselective membranes and by countercurrent chromatography (CPC).

Synthesis and reactivity of bioactive heterocycles
We study new reactivity pathways for relevant heterocycles (pyridines, indoles, oxygen-heterocycles, etc.). Our main goal is to develop efficient synthetic methodologies for the preparation of bioactive compounds. Recently, we have started a project for the incorporation of N- and O-heterocycles in multi-component reactions. In these processes, several molecules react to afford a single product, thereby increasing molecular diversity and exploratory power. These features make this approach very powerful in the development of SAR studies of drug-like compounds.

Funding

This group receives financial support from the following sources:

  • Ministerio de Educación y Ciencia (MEC - Spanish Ministry of Science & Education)
More info

Scientific publications search

Scientific publications search


Research Directory

Core facilities and Services Directory

  • Generalitat de catalunya
  • Generalitat de catalunya. Salut
  • Universidad de Barcelona
  • Parc cientific

Institute for Research in Biomedicine (IRB Barcelona)
Parc Científic de Barcelona
C/ Baldiri Reixac 10-12
08028 Barcelona - Spain
Tel: (+34)93 403 7111 | Fax: +34 93 403 7114
infoarrobairbbarcelona.org