Elias Maccioni

 
 maccione

Elias Maccioni

Address: Dipartimento di Scienze della Vita e dell’Ambiente
Drug Science Unit – Università di Cagliari
Via Ospedale 72, 09124 Cagliari (Italy)
Phone: +39-070-6758744
Fax: +39-070-6758553
Email: macione@unica.it

Brief Curriculum Vitae

Elias Maccioni graduated at the University of Cagliari in 1990 and was appointed Assistant Professor of medicinal chemistry in 1992. In 1993-1994 he was visiting researcher at the Department of Chemistry of the University of Bangor, North Wales. In 2005 he was appointed Associate Professor of Medicinal Chemistry at the Faculty of Pharmacy of the University of Cagliari, Italy. He now leads the research group of Drug Discovery and Drug Synthesis at the University of Cagliari. Since the Academic Year 2009 he is coordinator of the PhD school of “Pharmaceutical Sciences and Technologies at the University of Cagliari. He is also coordinator of the Paul Ehrlich European Medicinal Chemistry PhD Network for the University of Cagliari. Prof Maccioni is a member of the board of the “Life, Environmental and Drug Sciences” PhD program.
Since 1992 is a member of the Division of Medicinal Chemistry of the Italian Society of Chemistry.

Lines of research

The main theme of our research is the design and synthesis of enzyme inhibitors and modulators. In this respect, through a well-established interdisciplinary scientific network we dedicate our efforts to the rational design of small molecules, their synthesis and the comprehension of their mode of action.
Our interest is focused on the following research topics:

  • dual Inhibitors of HIV 1 Reverse Transcriptase;
  • identification and validation of druggable targets for EBOLA virus;
  • synthesis an structure activity relationships of carbonic anhydrase inhibitors isozymes;
  • identification of a “multidrug single molecule” (MSM) approach for neurodegenerative diseases;
  • synthesis and mode of action investigation of small molecules for the inhibition of C.albicans growth;
  • design, synthesis biophysical/biological evaluation of DNA G-quadruplex stabilisers as antitumor agents.

Collaborators and Collaborations

None of the above reported scientific investigation would have been possible, without the effective collaboration and friendship of all the research team members and extra-team scientists.
Team members: Dott. Simona Distinto, Dott Rita Meleddu, Dott. Giulia Bianco, Dott. Antonella Arridu, and Dott. Claudia Melis.
Extra-team scientists: Prof. Stefano Alcaro, Prof. Enzo Tramontano, Prof Filippo Cottiglia, Prof. Peter Matyus, Prof. Claudiu Supuran, Prof. Fernanda Borges, Prof Alessandro DeLogu, Prof. Claudia Sissi.

Most recent publications

  • Meleddu, R., Maccioni, E., Distinto, S., Bianco, G., Melis, C., Alcaro, S., Cottiglia, F., Ceruso, M., Supuran, C.T. New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII (2015) Bioorganic and Medicinal Chemistry Letters, . Article in Press.
  • Meleddu, R., Distinto, S., Corona, A., Bianco, G., Cannas, V., Esposito, F., Artese, A., Alcaro, S., Matyus, P., Bogdan, D., Cottiglia, F., Tramontano, E., Maccioni, E. (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro- 1H -indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase (2015) European Journal of Medicinal Chemistry, 93, pp. 452-460.
  • De Luca, M.A., Lai, F., Corrias, F., Caboni, P., Bimpisidis, Z., Maccioni, E., Fadda, A.M., Di Chiara, G. Lactoferrin- and antitransferrin-modified liposomes for brain targeting of the NK3 receptor agonist senktide: Preparation and in vivo evaluation (2015) International Journal of Pharmaceutics, 479 (1), pp. 129-137.
  • Ruiu, S., Anzani, N., Orrü, A., Floris, C., Caboni, P., Alcaro, S., Maccioni, E., Distinto, S., Cottiglia, F. Methoxyflavones from Stachys glutinosa with binding affinity to opioid receptors: In silico, in vitro, and in vivo studies (2015) Journal of Natural Products, 78 (1), pp. 69-76.
  • Rocca, R., Moraca, F., Costa, G., Alcaro, S., Distinto, S., Maccioni, E., Ortuso, F., Artese, A., Parrotta, L. Structure-based virtual screening of novel natural alkaloid derivatives as potential binders of h-telo and c-myc DNA G-quadruplex conformations (2015) Molecules, 20 (1), pp. 206-223.
  • Meleddu, R., Cannas, V., Distinto, S., Sarais, G., Del Vecchio, C., Esposito, F., Bianco, G., Corona, A., Cottiglia, F., Alcaro, S., Parolin, C., Artese, A., Scalise, D., Fresta, M., Arridu, A., Ortuso, F., Maccioni, E., Tramontano, E. Design, synthesis, and biological evaluation of 1,3-diarylpropenones as dual inhibitors of HIV-1 reverse transcriptase (2014) ChemMedChem, 9 (8), pp. 1869-1879.
  • Ruiu, S., Anzani, N., Orrù, A., Floris, C., Caboni, P., Maccioni, E., Distinto, S., Alcaro, S., Cottiglia, F. N-Alkyl dien- and trienamides from the roots of Otanthus maritimus with binding affinity for opioid and cannabinoid receptors (2013) Bioorganic and Medicinal Chemistry, 21 (22), pp. 7074-7082.
  • Distinto, S., Maccioni, E., Meleddu, R., Corona, A., Alcaro, S., Tramontano, E. Molecular aspects of the RT/drug interactions. Perspective of dual inhibitors (2013) Current Pharmaceutical Design, 19 (10), pp. 1850-1859. Cited 11 times.
  • Alcaro, S., Musetti, C., Distinto, S., Casatti, M., Zagotto, G., Artese, A., Parrotta, L., Moraca, F., Costa, G., Ortuso, F., Maccioni, E., Sissi, C. Identification and characterization of new DNA G-quadruplex binders selected by a combination of ligand and structure-based virtual screening approaches (2013) Journal of Medicinal Chemistry, 56 (3), pp. 843-855.
  • Cardia, M.C., Sanna, M.L., Meleddu, R., Distinto, S., Yañez, M., Viña, D., Lamela, M., Maccioni, E. A novel series of 3,4-disubstituted dihydropyrazoles: Synthesis and evaluation for MAO enzyme inhibition (2013) Journal of Heterocyclic Chemistry, 50 (SUPPL.1), pp. E87-E92.
  • Secci, D., Carradori, S., Bolasco, A., Bizzarri, B., D’Ascenzio, M., Maccioni, E. Discovery and optimization of pyrazoline derivatives as promising monoamine oxidase inhibitors (2012) Current Topics in Medicinal Chemistry, 12 (20), pp. 2240-2257.
  • Distinto, S., Esposito, F., Kirchmair, J., Cardia, M.C., Gaspari, M., Maccioni, E., Alcaro, S., Markt, P., Wolber, G., Zinzula, L., Tramontano, E. Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach (2012) European Journal of Medicinal Chemistry, 50, pp. 216-229.
  • Distinto, S., Yáñez, M., Alcaro, S., Cardia, M.C., Gaspari, M., Sanna, M.L., Meleddu, R., Ortuso, F., Kirchmair, J., Markt, P., Bolasco, A., Wolber, G., Secci, D., Maccioni, E. Synthesis and biological assessment of novel 2-thiazolylhydrazones and computational analysis of their recognition by monoamine oxidase B (2012) European Journal of Medicinal Chemistry, 48, pp. 284-295.
  • Maccioni, E., Alcaro, S., Cirilli, R., Vigo, S., Cardia, M.C., Sanna, M.L., Meleddu, R., Yanez, M., Costa, G., Casu, L., Matyus, P., Distinto, S. 3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B (2011) Journal of Medicinal Chemistry, 54 (18), pp. 6394-6398.
  • Dunkel, P., Balogh, B., Meleddu, R., Maccioni, E., Gyires, K., Mátyus, P. Semicarbazide-sensitive amine oxidase/vascular adhesion protein-1: A patent survey (2011) Expert Opinion on Therapeutic Patents, 21 (9), pp. 1453-1471.
  • Maccioni, E., Alcaro, S., Orallo, F., Cardia, M.C., Distinto, S., Costa, G., Yanez, M., Sanna, M.L., Vigo, S., Meleddu, R., Secci, D. Synthesis of new 3-aryl-4,5-dihydropyrazole-1-carbothioamide derivatives. An investigation on their ability to inhibit monoamine oxidase (2010) European Journal of Medicinal Chemistry, 45 (10), pp. 4490-4498.
  • Chimenti, F., Secci, D., Bolasco, A., Chimenti, P., Granese, A., Carradori, S., Maccioni, E., Cardia, M.C., Yáñez, M., Orallo, F., Alcaro, S., Ortuso, F., Cirilli, R., Ferretti, R., Distinto, S., Kirchmair, J., Langer, T. Synthesis, semipreparative HPLC separation, biological evaluation, and 3D-QSAR of hydrazothiazole derivatives as human monoamine oxidase B inhibitors (2010) Bioorganic and Medicinal Chemistry, 18 (14), pp. 5063-5070.
  • Sanna, M.L., Maccioni, E., Vigo, S., Faggi, C., Cirilli, R. Application of an immobilised amylose-based chiral stationary phase to the development of new monoamine oxidase B inhibitors (2010) Talanta, 82 (1), pp. 426-431.
  • Cirilli, R., Fiore, S., La Torre, F., Maccioni, E., Secci, D., Sanna, M.L., Faggi, C. Semipreparative HPLC enantioseparation, chiroptical properties, and absolute configuration of two novel cyclooxygenase-2 inhibitors (2010) Chirality, 22 (1), pp. 56-62.
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