SinFarm (CHIM/08)

Attività di ricerca

Our research focuses on developing innovative tools to combat infectious diseases and we are currently involved in three different research programs:

With the emergence of resistant M. tuberculosis strains, co-infection with HIV, and the existence of latent tuberculosis infections, our medicinal chemistry program aims at identifying new anti-TB drugs that target both drug-susceptible and drug-resistant M. tuberculosis strains, that are compatible with ART and kill the bug in its different physiological states, including latent ones.

Despite substantial progress in the field, malaria remains a global health issue and currently available control strategies are not sufficient to achieve eradication, Therefore, there is an imperative need to enrich the drug discovery pipeline, preferably with curative compounds that can also act prophylactically. Agents able to prevent transmission are likely to have a strong impact on malaria. Our medicinal chemistry campaign aims at identifying novel drugs targeting sexual stages of Plasmodium and innovative methods to target malaria transmission from host to vector, and vice versa.

Coxsackievirus A9 (CVA9) and Coxsackievirus B3 (CVB3) are both serotypes belonging to the enterovirus B species. Although CVA9 infection often leads to mild symptoms, it has also been the cause of a meningitis outbreak as well as found to cause hepatitis. CVB3 in turn is more associated with myocarditis, pancreatitis and meningitis, with the infection having been observed to be particularly prevalent in the heart and pancreas. Besides vaccines, development of effective antivirals is the only alternative. Therefore, further efforts are needed to develop novel antivirals, and our medicinal chemistry program aims at designing new and potent phenylbenzamides, identified through a screening of an in-house library of 201 compounds of diverse chemical scaffolds against CVA9 and CVB3.

Collaborazioni nazionali e internazionali
  • Flaminia Catteruccia (Harvard T.H. Chan School of Public Health, USA)
  • Musa Mhlanga (University of Cape Town, South Africa)
  • Kelly Chibale (University of Cape Town, South Africa)
  • Lyn-Marié Birkholtz (University of Pretoria, South Africa)
  • Varpu Marjomäki (University of Jyväskylä, Finland)
  • Alessandro De Logu (Università degli Studi di Cagliari, Italy)

lab fully equipped for organic synthesis, access to NMR departmental facilities

Settori ERC

LS7_3 - Pharmacology, pharmacogenomics, drug discovery and design, drug therapy

  • 2020- Progetti di Ricerca Universitari: " Nuovi derivati pirazolici come potenziali agenti anti-tubercola
  • 2019- Progetti di Ricerca Universitari: “Nuovi derivati tri-antranilati come potenziali agenti anti-tubercolari”
  • 2017- Grandi Ricerche Universitarie: “Novel MmpL3 inhibitors-loaded niosomes to treat tuberculosis via lung delivery”
  • 2016- Grandi Ricerche Universitarie: "Novel MmpL3 inhibitors to treat tuberculosis”
  • 2015- Progetti di Ricerca Universitari: “Targeting tryptophan biosynthesis to treat tuberculosis

Publications (2019-2021)

  1. Consalvi, S., Venditti, G., Zhu, J., Boshoff, H.I., Arora, K., De Logu, A., Ioerger, T.R., Rubin, E.J., Biava, M., Poce, G. 6-Fluorophenylbenzohydrazides inhibit Mycobacterium tuberculosis growth through alteration of tryptophan biosynthesis (2021) Eur. J. Med. Chem., 226, 113843. DOI: 10.1016/j.ejmech.2021.113843
  2. Appetecchia, F., Consalvi, S., Berrino, E., Gallorini, M., Granese, A., Campestre, C., Carradori, S., Biava, M., Poce, G. A novel class of dual-acting DCH-CORMs counteracts oxidative stress-induced inflammation in human primary tenocytes (2021) Antioxidants, 10 (11), 1828. DOI: 10.3390/antiox10111828
  3. Spano, M., Maccelli, A., Matteo, G.D., Ingallina, C., Biava, M., Crestoni, M.E., Bardaud, J.-X., Giusti, A.M., Mariano, A., D’abusco, A.S., Sobolev, A.P., Lasalvia, A., Fornarini, S., Mannina, L. Metabolomic profiling of fresh goji (Lycium barbarum l.) berries from two cultivars grown in central italy: A multi-methodological approach (2021) Molecules, 26 (17), 5412.  DOI: 10.3390/molecules26175412
  4. Aiello, P., Consalvi, S., Poce, G., Raguzzini, A., Toti, E., Palmery, M., Biava, M., Bernardi, M., Kamal, M.A., Perry, G., Peluso, I. Dietary flavonoids: Nano delivery and nanoparticles for cancer therapy (2021) Semin. Cancer Biol., 69, 150-165. DOI: 10.1016/j.semcancer.2019.08.029
  5. Consalvi, S., Poce, G., Ghelardini, C., Di Cesare Mannelli, L., Patrignani, P., Bruno, A., Anzini, M., Calderone, V., Martelli, A., Testai, L., Giordani, A., Biava, M. Therapeutic potential for coxibs-nitric oxide releasing hybrids in cystic fibrosis (2021) Eur. J. Med. Chem., 210, 112983, DOI: 10.1016/j.ejmech.2020.112983
  6. Consalvi, S., Poce, G., Scarpecci, C., Biava, M. Overcoming drug resistance in TB: An update (2020) Future Microbiol., 15 (17), 1607-1609. DOI: 10.2217/fmb-2020-0089
  7. Appetecchia, F., Consalvi, S., Scarpecci, C., Biava, M., Poce, G. SAR analysis of small molecules interfering with energy-metabolism in Mycobacterium tuberculosis (2020) Pharmaceuticals, 13 (9), 1-33. DOI: 10.3390/ph13090227
  8. Consalvi, S., Scarpecci, C., Biava, M., Poce, G. Mycobacterial tryptophan biosynthesis: A promising target for tuberculosis drug development? (2019) Bioorg. Med. Chem. Lett., 29 (23), 126731. DOI: 10.1016/j.bmcl.2019.126731
  9. Poce, G., Consalvi, S., Venditti, G., Alfonso, S., Desideri, N., Fernandez-Menendez, R., Bates, R.H., Ballell, L., Barros Aguirre, D., Rullas, J., De Logu, A., Gardner, M., Ioerger, T.R., Rubin, E.J., Biava, M. Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis (2019) ACS Med. Chem. Lett., 10 (10), 1423-1429. DOI: 10.1021/acsmedchemlett.9b00204
  10. Guglielmi, P., Carradori, S., Campestre, C., Poce, G. Novel therapies for glaucoma: a patent review (2013-2019) (2019) Expert Opin. Ther. Pat., 29 (10), 769-780. DOI: 10.1080/13543776.2019.1653279
  11. Raguzzini, A., Poce, G., Consalvi, S., Toti, E., Palmacci, F., Biava, M., Peluso, I. Chocolate consumers and lymphocyte-to-monocyte ratio: A working hypothesis from a preliminary report of a pilot study in celiac subjects (2019) Antioxidants, 8 (10), 440. DOI: 10.3390/antiox8100440
  12. Palmacci, F., Toti, E., Raguzzini, A., Catasta, G., Aiello, P., Peluso, I., Biava, M., Palmery, M. Neutrophil-to-lymphocyte ratio, Mediterranean diet, and bone health in coeliac disease patients: A pilot study (2019) Oxid. Med. Cell. Longev., 2019, 7384193. DOI: 10.1155/2019/7384193
  Pubblicazioni 2010-2018
  1. Biava M Introduction to COX inhibitors, Future Medicinal Chemistry, 10, 1737-1740, 2018.
  2. Cheleschi S, Calamia V, Fernandez-Moreno M, Biava M, Giordani A, Fioravanti A, Anzini M, Blanco F In vitro comprehensive analysis of VA692 a new chemical entity for the treatment of osteoarthritis, International Immunopharmacology, 64, 86-100, 2018. 
  3. Poce G, Cocozza M, Alfonso S, Consalvi S, Venditti G, Fernandez-Menendez R, Bates RH, Barros Aguirre D, Ballell L, De Logu A, Vistoli G, Biava M In vivo potent BM635 analogue with improved drug-like properties, European J Med Chem, 145, 539-550, 2018.
  4. Venditti G, Poce G, Consalvi S, Biava M 1,5-Diarylpyrroles as potent antitubercular and anti-inflammatory agents, Chemistry of Heterocyclic Compounds, 1-11, 2017
  5. Poce G, Consalvi S, Cocozza M, Fernandez-Menendez R, Bates RH, Ortega Muro F, Barros Aguirre D, Ballell L, Biava M Pharmaceutical salt of BM635 with improved bioavailability, European Journal of Pharmaceutical Sciences 99, 17-23, 2017
  6. Consalvi S, Biava M, Poce G A series of COX-2 inhibitors endowed with NO-releasing properties: synthesis, biological evaluation and docking analysis. ChemMedChem  11, 1804-1811, 2016
  7. Di Capua A, Sticozzi C, Brogi S, Brindisi M,  Cappelli A,  Sautebin L,  Rossi A,  Pace S,  Ghelardini C,  Di Cesare Mannelli L,  Valacchi G,  Giorgi G,  Giordani A,  Poce G,  Biava M,  Anzini, M  Synthesis and biological evaluation of fluorinated 1,5-diarylpyrrole-3-alkoxyethyl ether derivatives as selective COX-2 inhibitors endowed with anti-inflammatory activity. European J Med Chem, 109, 99-106, 2016.
  8. Desideri N, Proietti Monaco L, Fioravanti R, Biava M, Yáñez M, Alcaro S, Ortuso F (E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors. European J Med Chem, 117, 292–300, 2016
  9. Poce G, Consalvi S, Biava M MmpL3 inhibitors: diverse chemical scaffolds inhibit the same target.      Mini Rev Med Chem. 16, 1274-1283, 2016
  10. Consalvi S, Biava M, Poce G COX inhibitors: a patent review (2011 - 2014). Expert Opin Ther Pat 25, 1357-71, 2015Poce G, Biava M Overcoming drug resistance for tuberculosis. Future Microbiology 10, 1735–1741, 2015
  11. Poce G, Biava M Overcoming drug resistance for tuberculosis. Future Microbiology 10,1735-1741, 2015
  12. Fioravanti R, Desideri N, Biava M, Droghini P, Atzori EM, Ibba C, Collu G, Sanna G, Delogu I, Loddo R, N-((1,3-Diphenyl-1H-pyrazol-4-yl)methyl)anilines: A novel class of anti-RSV agents. Bioorg Med Chem Lett.  25, 2401-2404, 2015
  13. Cheleschi S, Pascarelli NA, Valacchi G, Di Capua A, Biava M, Belmonte G, Giordani A, Sticozzi C, Anzini M, Fioravanti A Chondroprotective effect of three different classes of anti-inflammatory agents on human osteoarthritic chondrocytes exposed to IL-1β.Int Immunopharmacol, 28, 794-801, 2015
  14. Piccaro G, Poce G, Biava M, Giannoni F, Fattorini L Activity of lipophilic and hydrophilic drugs against dormant and replicating Mycobacterium tuberculosis. Journal of Antibiotics, 68, 711-714, 2015
  15. Dragset Marte S, PoceG, Alfonso S, Padilla-Benavides T, Ioerger T R, Kaneko T, Sacchettini JC, Biava M, Parish T, Argüello JM, Steigedal M, Rubin EJ, A Novel Antimycobacterial Compound Acts as an Intracellular Iron Chelator. AAC, 59, 2256-64, 2015.
  16. Consalvi S, Alfonso S, Di Capua A, Poce G, Pirolli A, Sabatino M, Ragno R, Anzini M, Sartini S, La Motta C, Ghelardini C, Di Cesare Mannelli L, Ghelardini C,  Biava M Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors. Bioorg Med Chem, 23, 810–820, 2015.
  17. Poce G, Cocozza M, Consalvi S, Biava M SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development. Eur J Med Chem, 86, 335-351, 2014.
  18. Biava M, Battilocchio C, Poce G, Alfonso S, Porretta GC, Consalvi S, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Ghelardini C, Di Cesare Mannelli L, Giordani A, Patrignani P, Anzini M Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors. Bioorg Med Chem, 22,  772–786, 2014
  19. Martelli A, Testai L, Anzini M, Cappelli A, Di Capua A, Biava M, Poce G, Consalvi S, Giordani A, Caselli G, Rovati L, Ghelardini C, Patrignani P, Sautebin L, Breschi MC, Calderone V The novel anti‐Inflammatory agent VA694, endowed with both NO‐Releasing and COX2‐selective inhibiting properties, exhibits NO‐mediated positive effects on blood pressure, coronary flow and endothelium in an experimental model of hypertension and endothelial dysfunction. Pharmacol Research, 78, 1– 9, 2013.
  20. Radi M, Bernardo V, Vignaroli G, Brai A, Biava M, Schenone S, Botta M An alternative synthetic approach for the synthesis of biologically relevant 1,4-disubstituted pyrazolo[3,4-d]pyrimidines. Tetrahedron Lett, 54, 5204-5206, 2013.
  21. Fioravanti R, Desideri N, Biava M, Proietti Monaco L, Grammatica L, Yàñez M Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles. Bioorg Med Chem Lett, 23, 5128-5130, 2013.
  22. Tintori C,  Laurenzana I, La Rocca F,  Falchi F, Carraro F, Ruiz A, Esté JA, Kissova M, Crespan E, Maga G, Biava M, Brullo C, Schenone S, Botta M Identification of Hck inhibitors as hits for the development of antileukemia and anti-HIV agents. ChemMedChem, 8, 1353-1360, 2013.
  23. Battilocchio C, Guetzoyan L, Cervetto C,  Di Cesare Mannelli L, Frattaroli D, Baxendale IR, Maura G, Rossi A, Sautebin L, Biava M, Ghelardini C, Marcoli M, Ley SV Flow synthesis and bio-pharmacological studies of an adamantane derivative that shows analgesic activity and inhibits the P2X7-evoked glutamate release. ACS Med Chem Lett, 4, 704-709, 2013.
  24. Friggeri L, Ballante F, Ragno R, Musmuca I, De Vita D, Manetti F, Biava M, Scipione L, Di Santo R, Costi R, Feroci M, Tortorella S Pharmacophore assessment through 3-D QSAR: evaluation of the predictive ability on new derivatives by the application on a serie of antitubercular agents. J Chem Inf Model, 53, 1463-1474, 2013.
  25. Mazzarino M,  Biava M, de la Torre X, Fiacco I, Botrè F  Characterization of the biotransformation pathways of clomiphene, tamoxifen and toremifene as assessed by LC-MS/(MS) following in vitro and excretion studies. Anal Bioanal Chem, 405, 5467-5487, 2013.
  26. Baiocco P, Poce G, Alfonso S, Cocozza M, Porretta GC, Colotti G, Biava M, Moraca F, Botta M, Yardley V, Fiorillo A, Malatesta F,  Ilari A Evaluation of azole-based compounds as inhibitors of trypanothione reductase from leishmania infantum: a comparative analysis with its physiological substrate by X-ray crystallography. ChemMedChem, 8, 1175-1183, 2013.
  27. Battilocchio C, Poce G, Alfonso S, Porretta GC, Consalvi S, Sautebin L, Rossi A, Pace F, Ghelardini C, Di Cesare Mannelli L, Schenone S, Giordani A, Di Francesco L, Patrignani P,  Biava M  A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity. Bioorg Med Chem, 21, 3695-3701, 2013.
  28. Anzini M, Di Capua A, Valenti S, Brogi S, Rovini M, Giuliani G, Cappelli A, Vomero S, Chiasserini L, Saga A, Poce G, Giorgi G, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Papa G, Ghelardini C, Di Cesare Mannelli L, Benetti V, Giordani A, Anzellotti P, Dovizio M, Patrignani P, Biava M  Novel analgesic/anti-inflammatory agents: 1,5-diarylpyrrole nitro-oxyalkyl ethers and related compounds as cyclooxygenase-2 inhibiting nitric oxide donors.  J Med Chem, 56, 3191-3206, 2013.
  29. Sticozzi C, Belmonte G, Cervellati F, Di Capua A, Maioli E, Cappelli A, Giordani A, Biava M, Anzini M, Valacchi G Antiproliferative effect of two novel COX-2 inhibitors on human keratinocytes. Eur J Pharm Sci,  49, 133-141, 2013.
  30. Poce G, Bates HR, Alfonso S, Cocozza M,  Porretta GC, Ballel L,  Rullas J, De Logu A, Agus E, La Rosa V, Pasca MR, De Rossi E, Wae B, Franzblau SJ, Manetti F, Botta M, Biava M  Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection. Plos One, 8, e56980, 2013.
  31. Desideri N, Fioravanti R, Proietti Monaco L, Biava M, Yàñez M, Ortuso F, Alcaro S 1,5-Diphenylpenta-2,4-dien-1-ones as potent and selective monoamine oxidase-B inhibitors. Eur J Med Chem, 59, 91-100, 2013.
  32. Biava M,  Battilocchio C, Poce G, Alfonso S, Porretta GC, Consalvi S, Calderone V, Martelli A, Testai L, Ghelardini C, Di Cesare Mannelli L, Sautebin L, Rossi A, Giordani A, Patrignani P, Anzini M Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit Cycloxygenase-2 isoenzyme. Eur J Med Chem, 58, 287-298, 2012.
  33. Fioravanti A, Tinti A, Pascarelli A, Di Capua A, Lamboglia A, Cappelli A, Biava M, Giordani A, Niccolini S, Galeazzi M, Anzini M In vitro effects of VA441, a new selective Cyclooxygenase-2 inhibitor, on human osteoarthritic chondrocytes exposed to IL-1β. J Pharmacol Sci, 120, 6-14, 2012.
  34. Battilocchio C, Baxendale IR, Biava M, Kitching MO, Ley SVA Flow based   synthesis of 2-aminoadamantane-2-carboxilic acid. Org Process Res Dev  16, 798-810, 2012.
  35. Battilocchio C, Baumann M, Baxendale IR, Biava M, Kitching MO, Ley SV, Martin  RE, Ohnmacht SA, Tappina NDC Scale-Up of flow-assisted synthesis of C2-symmetric chiral PyBox ligands. Synthesis, 44, 635–647, 2012.
  36. La Rosa V, Poce G, Ortiz Canseco J, Buroni S, Pasca MR, Biava M, Raju RM, Porretta GC, Alfonso S, Battilocchio C, Javid B, Sorrentino F, Ioerger TR, Sacchettini JC, Manetti F,  Botta M, De Logu A, Rubin EJ MmpL3 is the cellular target of the antitubercular pyrrole derivative BM212. AAC, 56, 324–331, 2012.
  37. Biava M, Porretta GC, Poce G, Battilocchio C, Alfonso S, Rovini M, Valenti S, Giorgi G, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Papa G, Ghelardini C, Di Cesare Mannelli L, Giordani A, Anzellotti P, Bruno A, Patrignani P, Anzini M Novel analgesic/anti-inflammatory agents: diarylpyrrole acetic esters endowed with nitric oxide releasing properties. J Med Chem, 54, 7759−7771, 2011.
  38. Radi M, Brullo C, Crespan E, Tintori C, Musumeci F, Biava M, Schenone S, Dreassi E, Zamperini C, Maga G, Pagano D, Angelucci A, Bologna M, Botta M Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells. Bioorg Med Chem Lett  21, 5928-5933, 2011.
  39. Schenone S, Brullo C, Musumeci F, Biava M, Falchi F, Botta M Fyn kinase in brain diseases and cancer: the search for inhibitors. Current Med Chem,  18,  2921-2942, 2011.
  40. Maccari G, Jaeger T, Moraca F, Biava M, Flohe L, Botta M A fast virtual screening approach to identify structurally diverse inhibitors of trypanothione reductase. Bioorg Med Chem Lett, 21,  5255-5258, 2011.
  41. Biava M, Porretta GC, Poce G, Battilocchio C, Botta M, Manetti F, Rovini M, Cappelli A, Sautebin L, Rossi A, Pergola C, Ghelardini C, Galeotti N, Makovec F, Giordani A, Anzellotti P, Tacconelli S, Patrignani P, Anzini M Enlarging the NSAIDs family: ether, ester and acid derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents. Curr Med Chem, 18, 1540-1554, 2011.
  42. Biava M, Porretta GC, Poce G, Battilocchio C, Alfonso S, De Logu A, Manetti F, Botta M Developing pyrrole-derived antimycobacterial agents: a rational lead optimization approach. ChemMedChem, 6, 593-599, 2011.
  43. Biava M, Porretta GC, Poce G, Battilocchio C, Alfonso S, De Logu A, Serra N, Manetti F, Botta M Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin. Bioorg Med Chem, 18, 8076–8084, 2010.
  44. Biava M, Porretta GC, Poce G, Battilocchio C, Manetti F, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Norcini M, Makovec F,  Anzellotti P, Cirilli R, Ferretti R, Patrignani P, Anzini M Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis, in vitro and in vivo biological evaluation. J Med Chem, 53, 723-733, 2010.

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