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Research Unit coordinated by Prof. Carlo De Micheli  

Academic staff: Prof. Carlo De Micheli,Prof. Paola Conti, Dr. Andrea Pinto, Dr. Lucia Tamborini

Research Collaborators: Dott.ssa Roberta Ettari, Dott.ssa Federica Mastronardi

The research group has complementary skills in medicinal chemistry, synthetic organic chemistry and analysis. Research interests are focused on the following subjects:

1) Design and synthesis of biologicaly active unnatural amino acids

The research group is specialized in the design, synthesis and study of the structure-activity relationship of conformationally constrained analogues of endogenous amino acids (glutamate, aspartate, GABA and glutamine).

At present, the main research lines are:

a) New ligands of GABA and Glu receptors as anticonvulsant and neuroprotective agents.

b) PET ligands for CNS imaging applications

c) Excitatory amino acid transporter inhibitors as a new approach for the treatment of cerebral ischemia

d) Inhibitors of glutamine-dependent enzymes involved in amino acid and nucleotide biosynthesis.

2) Design of covalent enzymatic inhibitors

Within the framework of a project aimed at the discovery of new chemotherapeutic agents for the treatment of parasitic diseases, such as African trypanosomiasis, malaria and leishmaniosis, we develop covalent inhibitors able to selectively inactivate enzymes crucial for parasite replication and survival in the human host.

3) Innovative Synthetic Technologies

The research group is engaged in the development of flow-based processes, combined with the use of immobilized reagents, scavengers and catalysts, for the purification-free synthesis of libraries of compounds and for the multi-step synthesis of complex biologically active molecules. This modern technology enables a significant reduction of reaction time and costs and is more environmentally friendly due to minimization of waste production.

We also exploit this methodology for the kinetic resolution of chiral substrates using biocatalysts (polymer-supported enzymes or whole-cells).

4) Application of analytical techniques

The research group studies the use of chromatographic techniques for the determination of the enantiomeric composition of chiral ligands and for the separation on a preparative scale of pure enantiomers starting from racemic mixtures.

National and international collaborations

The research projects outlined above are realized in collaboration with the following institutions: Department of Drug Design and Pharmacology – University of Copenhagen; Johns Hopkins University; Cornell University; Glasgow Biomedical Research Centre; Istituto Mario Negri; University of Milano, Messina, Pavia, Parma, Modena, Napoli and Siena.

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