Seven-Lab (CHIM/08)

Attività di ricerca

The research activities of the SevenLab group are mainly developed on three lines:

  1. Synthesis and biological evaluation of multifactorial Cholinesterase inhibitors, endowed with antioxidant, metal-chelating properties and with anti-aggregation activity vs β-amyloid peptide;
  2. Synthesis of anti-fungal agents belonging to azole class and s anti-biofilm agents to the classes of indole and cinnamic derivatives;
  3. Synthesis of indole and azole derivatives as anti-parasitic agents, in particular anti-trypanposomal and anti-Leishmanial compounds.
Collaborazioni nazionali e internazionali
  • Prof. Reto Brun, "Department Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute", Basel, Switzerland;
  • Prof. Louis Maes "Laboratory for Microbiology, Parasitology and Hygiene (LMPH)" Antwerp University, Belgium;
  • Prof. Carlos Alberto Montanari, "Departamento de Quimica e Fisica Molecular" Insitute of Chemistry of Sao Carlos, Universiy of Sao Paulo, Brasil;
  • Prof.ssa Ana Marisa Fusco Almeida, Department of ClinicalAnalysis, Sao Paulo State University, Araraquara, Brasil;
  • Prof.Maurizio Botta, Dipartimento di Biotecnologie, Chimica e Farmacia University of Siena, Italy;
  • Prof. Alessandro De Logu, Dipartimento di Scienze della Vita e dell’Ambiente, University of Cagliari, Italy;
  • Manuela Bartolini, Dipartimento di Farmacia e Biotecnologie, University of Bologna, Italy;
  • Prof. Stefano Alcaro, Dipartimento di Scienze Farmacobiologiche University "Magna Græcia", Catanzaro, Italy;
  • Dott.ssa Giovanna Simonetti, Dipartimento di Sanità Pubblica e Malattie Infettive, “Sapienza” University of Rome, Italy.
  • Prof.ssa Marta Feroci, Dipartimento di Scienze di Base e Applicate per l’Ingegneria, “Sapienza” University of Rome, Italy.
Strumentazione

SevenLab is equipped for traditional chemical synthesis and has free access to microwave assisted chemical synthesis instrument. The lab is also equipped for purification with chromatographic techniques including flash and HPLC) and for spectroscopic characterization of synthesized compound (FT-IR, UV-Vis, LC-MS) and has access to Department NMR instrument.

Settori ERC
  • LS6_11 - Prevention and treatment of infection by pathogens (e.g. vaccination, antibiotics, fungicide)
  • LS6_7 - Microbiology
  • LS7_3 - Pharmacology, pharmacogenomics, drug discovery and design, drug therapy
Finanziamenti

Anno 2016 - progetto di Ateneo- New azole derivatives as antifungal and antiprotozoal agents;

Pubblicazioni

Publications (2015-2018):

1. Poongavanam, V.; Corona, A.; Steinmann, C.; Scipione, L.; Grandi, N.; Pandolfi, F.; Di Santo, R.; Costi, R.; Esposito, F.; Tramontano, E.; Kongsted, J.
Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: Binding mode insights through magnesium complexation and site-directed mutagenesis studies
(2018) MedChemComm 9(3) 562-575.
DOI: 10.1039/c7md00600d

 2. Pandolfi, F., De Vita, D., Bortolami, M., Coluccia, A., Di Santo, R., Costi, R., Andrisano, V., Alabiso, F., Bergamini, C., Fato, R., Bartolini, M., Scipione, L
New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation
(2017) European Journal of Medicinal Chemistry 141, 197-210
DOI: 10.1016/j.ejmech.2017.09.022

3. De Vita, D., Angeli, A., Pandolfi, F., Bortolami, M., Costi, R., Di Santo, R., Suffredini, E., Ceruso, M., Del Prete, S., Capasso, C., Scipione, L., Supuran, C.T.
Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties
(2017) Journal of Enzyme Inhibition and Medicinal Chemistry 32(1) 798-804
DOI: 10.1080/14756366.2017.1327522

4. Madia, V.N., Benedetti, R., Barreca, M.L., Ngo, L., Pescatori, L., Messore, A., Pupo, G., Saccoliti, F., Valente, S., Mai, A., Scipione, L., Zheng, Y.G., Tintori, C., Botta, M., Cecchetti, V., Altucci, L., Di Santo, R., Costi, R.
Structure–Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase
(2017) ChemMedChem Volume 12(16), 1359-1368
DOI: 10.1002/cmdc.201700040

5. Saccoliti, F., Angiulli, G., Pupo, G., Pescatori, L., Madia, V.N., Messore, A., Colotti, G., Fiorillo, A., Scipione, L., Gramiccia, M., Di Muccio, T., Di Santo, R., Costi, R., Ilari, A.
Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivative
(2017) Journal of enzyme inhibition and medicinal chemistry 32(1), 304-310
DOI: 10.1080/14756366.2016.1250755

6. De Vita, D., Pandolfi, F., Ornano, L., Feroci, M., Chiarotto, I., Sileno, I., Pepi, F., Costi, R., Di Santo, R., Scipione, L.
New N,N-dimethylcarbamate inhibitors of acetylcholinesterase: design synthesis and biological evaluation
(2016) Journal of Enzyme Inhibition and Medicinal Chemistry, 26(24), 5931-5935.
DOI: 10.1080/14756366

7. De Vita, D., Simonetti, G., Pandolfi, F., Costi, R., Di Santo, R., D'Auria, F.D., Scipione, L.
Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans
(2016) Bioorganic and medicinal chemistry letters, 26 (24), 5931-5935
DOI: 10.1016/j.bmcl.2016.10.091

8. Schmid, T., Blees, J.S., Bajer, M.M., Wild, J., Pescatori, L., Cuzzucoli Crucitti, G., Scipione, L., Costi, R., Henrich, C.J., Brüne, B., Colburn, N.H., Di Santo, R.
Diaryl disulfides as novel stabilizers of tumor suppressor Pdcd4
(2016) PLoS ONE, 11(3), Article number e0151643.
DOI: 10.1371/journal.pone.0151643

9. De Vita, D., Pandolfi, F., Cirilli, R., Scipione, L., Di Santo, R., Friggeri, L., Mori, M., Fiorucci, D., Maccari, G., Christopher, R.S.A., Zamperini, C., Pau, V., De Logu, A., Tortorella, S., Botta, M.
Discovery of in vitro antitubercular agents through in silico ligand-based approaches
(2016) European Journal of Medicinal Chemistry, 121, pp. 169-180.
DOI: 10.1016/j.ejmech.2016.05.032

10. De Vita, D., Moraca, F., Zamperini, C., Pandolfi, F., Di Santo, R., Matheeussen, A., Maes, L., Tortorella, S., Scipione, L.
In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51
(2016) European Journal of Medicinal Chemistry, 113, pp. 28-33.
DOI: 10.1016/j.ejmech.2016.02.028

11. D'Ascenzio, M., Chimenti, P., Gidaro, M.C., De Monte, C., De Vita, D., Granese, A., Scipione, L., Di Santo, R., Costa, G., Alcaro, S., Yáñez, M., Carradori, S.
(Thiazol-2-yl)hydrazone derivatives from acetylpyridines as dual inhibitors of MAO and AChE: Synthesis, biological evaluation and molecular modeling studies
(2015) Journal of Enzyme Inhibition and Medicinal Chemistry, 30 (6), pp. 908-919.
DOI: 10.3109/14756366.2014.987138

12. Cuzzucoli Crucitti, G., Pescatori, L., Messore, A., Madia, V.N., Pupo, G., Saccoliti, F., Scipione, L., Tortorella, S., Di Leva, F.S., Cosconati, S., Novellino, E., Debyser, Z., Christ, F., Costi, R., Di Santo, R.
Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75
(2015) European Journal of Medicinal Chemistry, 101, art. no. 7963, pp. 288-294. Cited 2 times.
DOI: 10.1016/j.ejmech.2015.06.036

13. Pescatori, L., Métifiot, M., Chung, S., Masoaka, T., Cuzzucoli Crucitti, G., Messore, A., Pupo, G., Madia, V.N., Saccoliti, F., Scipione, L., Tortorella, S., Di Leva, F.S., Cosconati, S., Marinelli, L., Novellino, E., Le Grice, S.F.J., Pommier, Y., Marchand, C., Costi, R., Di Santo, R.
N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase
(2015) Journal of Medicinal Chemistry, 58 (11), pp. 4610-4623. Cited 3 times.
DOI: 10.1021/acs.jmedchem.5b00159

14. Cuzzucoli Crucitti, G., Métifiot, M., Pescatori, L., Messore, A., Madia, V.N., Pupo, G., Saccoliti, F., Scipione, L., Tortorella, S., Esposito, F., Corona, A., Cadeddu, M., Marchand, C., Pommier, Y., Tramontano, E., Costi, R., Di Santo, R.
Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain
(2015) Journal of Medicinal Chemistry, 58 (4), pp. 1915-1928. Cited 4 times.
DOI: 10.1021/jm501799k

15. Friggeri, L., De Vita, D., Pandolfi, F., Tortorella, S., Costi, R., Di Santo, R., Scipione, L.
Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors
(2015) Journal of Enzyme Inhibition and Medicinal Chemistry, 30 (1), pp. 166-172.
DOI: 10.3109/14756366.2013.866657

16. Mellini, P., De Vita, D., Di Rienzo, B., La Rosa, S., Padova, A., Scipione, L., Tortorella, S., Friggeri, L.
Efficient synthesis of 3,5-dicarbamoyl-1,4-dihydropyridines from pyridinium salts: Key molecules in understanding NAD(P)+/NAD(P)H pathways
(2015) Journal of Heterocyclic Chemistry, 52 (1), pp. 221-226.
DOI: 10.1002/jhet.

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