Alessandro BONARDI

Ruolo attuale:: Ricercatore Legge 240/10 a tempo determinato
SSD:: CHEM-07/A - Chimica farmaceutica
Afferenza organizzativa:: Dipartimento di Neuroscienze, Psicologia, Area del Farmaco e Salute del Bambino (NEUROFARBA)

Recapiti

alessandro.bonardi(AT)unifi.it

Alessandro BONARDI

Biografia

Nato a Firenze il 06/11/1991.

Laurea in Chimica e Tecnologia Farmaceutiche (voto 110): Università degli Studi di Firenze, 2016.

Dottorato di ricerca cum laude in Area del Farmaco e Trattamenti Innovativi (SSD CHEM-07/A), Università degli Studi di Firenze, 2021.

Ricercatore a Tempo Determinato di tipo A presso Università degli Studi di Firenze dal 2022.

Alessandro BONARDI

Curriculum

PERCORSO FORMATIVO

Dicembre 2016: Laurea Magistrale a ciclo unico in Chimica e Tecnologia Farmaceutiche, Università degli Studi di Firenze.

Titolo della Tesi: “Structural investigation of coumarin derivatives for the development of new potent Carbonic Anhydrase IX and XII inhibitors”. Relatore: Prof.ssa Vittoria Colotta; Correlatore: Prof.ssa Flavia Varano.

Votazione: 110/110.

Novembre 2017 – Ottobre 2020: Dottorato di Ricerca (PhD) in Area del Farmaco e Trattamenti Innovativi – curriculum Scienze Farmaceutiche (XXXIII ciclo). SSD CHIM/08. Dipartimento NEUROFARBA, Università degli Studi di Firenze.

Titolo della Tesi: “In silico strategies for the rational design, synthesis and biological evaluation of ligands targeting macromolecules of pharmaceutical interest”. Tutor Scientifico: Prof.ssa Paola Gratteri; Tutor Teorico: Prof. Claudiu T. Supuran.

Gennaio 2020 – Marzo 2020: Periodo di dottorato a Vienna presso il gruppo di ricerca del Prof. Vittorio Pace, Pharmaziezentrum, Universität Wien, 1090, Austria.

Febbraio 2021: Conseguimento del titolo di Dottore di Ricerca cum laude.

ESPERIENZA PROFESSIONALE

Novembre 2020 – Dicembre 2022: Assegnista di ricerca presso il Dipartimento NEUROFARBA (Sezione di Farmaceutica e Nutraceutica), Università degli Studi di Firenze.

Dicembre 2022 – ad oggi: Ricercatore Universitario (RTDA) presso il Dipartimento NEUROFARBA (Sezione di Farmaceutica e Nutraceutica), Università degli Studi di Firenze.

ATTIVITÀ SCIENTIFICA

L’attività di ricerca del Dr. Bonardi (autore di > 60 publicazioni) si è principalmente rivolta alla progettazione in silico, sintesi e valutazione biologica di modulatori di target biologici di interesse farmaceutico tra cui enzimi, recettori accoppiati a proteine G (GPCR) ed acidi nuclei. Le linee di ricerca nelle quali il Dr. Bonardi è più attivo si concentrano su: ▪ vari aspetti dei metalloenzimi Anidrasi Carboniche (CA) come drug-target, spaziando dalla progettazione in silico, alla sintesi e valutazione della cinetica enzimatica per la determinazione del profilo di attivazione o inibizione di modulatori delle CA tramite tecnica Stopped-Flow; ▪ progettazione in silico e sintesi di ligandi delle PBP (Penicillin Binding Protein), di ribosomi, di recettori ionotropi GABAA e di GPCR, come i recettori β-adrenergici; ▪ progettazione/studi in silico, sintesi e valutazione delle modalità di interazione di ligandi con acidi nucleici in conformazione canonica (doppia elica) e non (G-quadruplex).

Ad oggi, l’attività di ricerca del Dr. Bonardi è orientata anche verso l’utilizzo dell’approccio multi-target per lo sviluppo e sintesi di derivati che fondono porzioni CA inibitorie con farmacofori tipici attivi su altri target. Al momento questo approccio è utilizzato per la progettazione, sintesi, e valutazione biologico/strutturale di ligandi intercalanti del G-quadruplex e per la progettazione e sintesi di agenti antibatterici, anti-Alzheimer e di antagonisti selettivi β3-adrenergici. In quest’ultimo caso la strategia dello Structure-Based Virtual Screening è stata usata per l’individuazione di hit compounds.

ATTIVITÀ DIDATTICA

da A.A. 2021-2022 ad oggi: modulo di insegnamento nel corso Molecular Modeling in Chimica Farmaceutica (3CFU) nell’ambito delle attività didattiche a scelta (ADE, attività didattica elettiva) per i Corsi di Laurea Magistrale a Ciclo Unico in LM13-Farmacia, Università degli Studi di Firenze.

da A.A. 2021-2022 ad oggi: modulo di insegnamento nel corso Analisi dei Medicinali I modulo II - LM13-Farmacia, Università degli Studi di Firenze.

da A.A. 2023-2024 ad oggi: modulo di insegnamento nel corso Chimica Farmaceutica Avanzata - LM13- Chimica e Tecnologia Farmaceutiche, Università degli Studi di Firenze.

Il Dr. Bonardi è inoltre componente delle commissioni d’esame dell’insegnamento di Chimica Farmaceutica e Tossicologica II - LM13-Farmacia, Università degli Studi di Firenze.

Alessandro BONARDI

Interessi

- Sviluppo di modulatori selettivi per le isoforme dell’anidrasi carbonica

- Sviluppo di composti multitarget per il trattamento di patologie multifattoriali (e.g. glaucoma, tumori, Alzheimer, malattie infiammatorie, infezioni, ecc.)

- Valutazione dell’attività dei modulatori dell’anidrasi carbonica attraverso studi di cinetica enzimatica

- Progettazione di farmaci in silico (Virtual Screening, Docking, Dinamica molecolare, Predizione delle proprietà ADMET)

Alessandro BONARDI

Note

alessandro.bonardi@unifi.it

Alessandro BONARDI

Pubblicazioni

Legenda

Contributo su rivista |

Articolo su libro |

Libro |

Contributo in atti di convegno (proceeding) |

Brevetto |

Curatela | Altro

Altro |

Tesi di Dottorato

Niccolò Paoletti, Paola Gratteri, Claudiu T. Supuran, Alessandro Bonardi, (2025). Computational approaches in drug discovery: strategies to address polypharmacology and the synthesis/optimization of lead compounds. (Tutor: Paola Gratteri, Claudiu T. Supuran, Alessandro Bonardi)

Alessio Nocentini, Anna Di Porzio, Alessandro Bonardi, Carla Bazzicalupi, Andrea Petreni, Tarita Biver, Silvia Bua, Simona Marzano, Jussara Amato, Bruno Pagano, Nunzia Iaccarino, Stefano De Tito, Stefano Amente, Claudiu T. Supuran, Antonio Randazzo, Paola Gratteri (2024). Development of a multi-targeted chemotherapeutic approach based on G-quadruplex stabilisation and carbonic anhydrase inhibition. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, pp. 2366236-2366260, ISSN:1475-6374 DOI

Giovannuzzi, Simone; Chavarria, Daniel; Provensi, Gustavo; Leri, Manuela; Bucciantini, Monica; Carradori, Simone; Bonardi, Alessandro; Gratteri, Paola; Borges, Fernanda; Nocentini, Alessio; Supuran, Claudiu T. (2024). Dual Inhibitors of Brain Carbonic Anhydrases and Monoamine Oxidase-B Efficiently Protect against Amyloid-β-Induced Neuronal Toxicity, Oxidative Stress, and Mitochondrial Dysfunction. JOURNAL OF MEDICINAL CHEMISTRY, vol. 67, pp. 4170-4193, ISSN:0022-2623 DOI

Bua, Silvia; Bonardi, Alessandro; Mük, Georgiana Ramona; Nocentini, Alessio; Gratteri, Paola; Supuran, Claudiu T. (2024). Benzothiadiazinone-1,1-Dioxide Carbonic Anhydrase Inhibitors Suppress the Growth of Drug-Resistant Mycobacterium tuberculosis Strains. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 25, pp. 0-0, ISSN:1422-0067 DOI

Marjan Sobati; Morteza Abdoli; Andrea Angeli; Alessandro Bonardi; Marta Ferraroni; Claudiu T Supuran; Raivis Žalubovskis (2024). Sulfonamide-incorporated bis(α-aminophosphonates) as promising carbonic anhydrase inhibitors: Design, synthesis, biological evaluation, and X-ray crystallographic studies. ARCHIV DER PHARMAZIE, pp. 1-11, ISSN:0365-6233 DOI

Morteza Abdoli; Alessandro Bonardi; Paola Gratteri; Claudiu T Supuran; Raivis Žalubovskis (2024). Synthesis, carbonic anhydrase inhibition studies and modelling investigations of phthalimide-hydantoin hybrids. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 39, pp. 1-9, ISSN:1475-6374 DOI

Nocentini A.; Costa A.; Bonardi A.; Ammara A.; Giovannuzzi S.; Petreni A.; Bartolucci G.; Rani B.; Leri M.; Bucciantini M.; Fernandez-Bolanos J.G.; Lopez O.; Passani M.B.; Provensi G.; Gratteri P.; Supuran C.T. (2024). Enhanced Recognition Memory through Dual Modulation of Brain Carbonic Anhydrases and Cholinesterases. JOURNAL OF MEDICINAL CHEMISTRY, vol. 67, pp. 16873-16898, ISSN:1520-4804 DOI

Al-Matarneh, Cristina M.; Pinteala, Mariana; Nicolescu, Alina; Silion, Mihaela; Mocci, Francesca; Puf, Razvan; Angeli, Andrea; Ferraroni, Marta; Supuran, Claudiu T.; Zara, Susi; Carradori, Simone; Paoletti, Niccolò; Bonardi, Alessandro; Gratteri, Paola (2024). Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety. JOURNAL OF MEDICINAL CHEMISTRY, vol. 67, pp. 3018-3038, ISSN:0022-2623 DOI

Giovannuzzi S.; Nikitjuka A.; Angeli A.; Smietana M.; Massardi M.-L.; Turati M.; Ronca R.; Bonardi A.; Nocentini A.; Ferraroni M.; Supuran C.T.; Winum J.-Y. (2024). Benzoxaborinine, New Chemotype for Carbonic Anhydrase Inhibition: Ex Novo Synthesis, Crystallography, In Silico Studies, and Anti-Melanoma Cell Line Activity. JOURNAL OF MEDICINAL CHEMISTRY, vol. 67, pp. 18221-18234, ISSN:1520-4804 DOI Accesso ONLINE all'editore

D'Agostino I.; Bonardi A.; Ferraroni M.; Gratteri P.; Angeli A.; Supuran C.T. (2024). Exploring the Polypharmacological Potential of PCI-27483: A Selective Inhibitor of Carbonic Anhydrases IX and XII. ACS MEDICINAL CHEMISTRY LETTERS, vol. 15, pp. 2042-2045, ISSN:1948-5875 DOI Accesso ONLINE all'editore

Nocentini, Alessio; Bonardi, Alessandro; Bazzicalupi, Carla; Alterio, Vincenzo; Esposito, Davide; Monti, Simona Maria; Smietana, Michael; De Simone, Giuseppina; Supuran, Claudiu T; Gratteri, Paola; Winum, Jean-Yves (2023). 6-Substituted Triazolyl Benzoxaboroles as Selective Carbonic Anhydrase Inhibitors: In Silico Design, Synthesis, and X-ray Crystallography. JOURNAL OF MEDICINAL CHEMISTRY, vol. 66, pp. 8118-8129, ISSN:0022-2623 DOI Accesso ONLINE all'editore

Angeli A.; Ferraroni M.; Bonardi A.; Supuran C.T.; Nocentini A. (2023). Diversely N-substituted benzenesulfonamides dissimilarly bind to human carbonic anhydrases: crystallographic investigations of N-nitrosulfonamides. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 2178430-2178430, ISSN:1475-6366 DOI

Ommi, Ojaswitha; Paoletti, Niccolò; Bonardi, Alessandro; Gratteri, Paola; Bhalerao, Harshada Anil; Sau, Shashikanta; Nanduri, Srinivas; Mohammed, Arifuddin; Kalia, Nitin Pal; Sonti, Rajesh; Supuran, Claudiu T; Yaddanapudi, Venkata Madhavi (2023). Exploration of 3-aryl pyrazole-tethered sulfamoyl carboxamides as carbonic anhydrase inhibitors. ARCHIV DER PHARMAZIE, vol. 356, pp. 0-0, ISSN:0365-6233 DOI

Peerzada, Mudasir Nabi; Vullo, Daniela; Paoletti, Niccolò; Bonardi, Alessandro; Gratteri, Paola; Supuran, Claudiu T; Azam, Amir (2023). Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors. ACS MEDICINAL CHEMISTRY LETTERS, vol. 14, pp. 810-819, ISSN:1948-5875 DOI

Begines, Paloma; Bonardi, Alessandro; Nocentini, Alessio; Gratteri, Paola; Giovannuzzi, Simone; Ronca, Roberto; Tavani, Camilla; Luisa Massardi, Maria; López, Óscar; Supuran, Claudiu T (2023). Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies. BIOORGANIC & MEDICINAL CHEMISTRY, vol. 94, pp. 117467-117482, ISSN:0968-0896 DOI

Sobati, Marjan; Abdoli, Morteza; Bonardi, Alessandro; Gratteri, Paola; Supuran, Claudiu T; Žalubovskis, Raivis (2023). Inhibition Profiles of Some Novel Sulfonamide-Incorporated α-Aminophosphonates on Human Carbonic Anhydrases. ACS MEDICINAL CHEMISTRY LETTERS, vol. 14, pp. 1067-1072, ISSN:1948-5875 DOI Accesso ONLINE all'editore

Abdoli, Morteza; Bonardi, Alessandro; Paoletti, Niccolò; Aspatwar, Ashok; Parkkila, Seppo; Gratteri, Paola; Supuran, Claudiu T; Žalubovskis, Raivis (2023). Inhibition Studies on Human and Mycobacterial Carbonic Anhydrases with N-((4-Sulfamoylphenyl)carbamothioyl) Amides. MOLECULES, vol. 28, pp. 0-0, ISSN:1420-3049 DOI Accesso ONLINE all'editore

Abdoli, Morteza; Krasniqi, Vesa; Bonardi, Alessandro; Gütschow, Michael; Supuran, Claudiu T; Žalubovskis, Raivis (2023). 4-Cyanamido-substituted benzenesulfonamides act as dual carbonic anhydrase and cathepsin inhibitors. BIOORGANIC CHEMISTRY, vol. 139, pp. 1-7, ISSN:1090-2120 DOI

Aspatwar, Ashok; Bonardi, Alessandro; Aisala, Heidi; Zueva, Ksenia; Primmer, Craig R; Lumme, Jaakko; Parkkila, Seppo; Supuran, Claudiu T (2023). Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6366 DOI

Ramzan, Farhat; Nabi, Syed Ayaz; Lone, Mehak Saba; Bonardi, Alessandro; Hamid, Aabid; Bano, Sameena; Sharma, Kalicharan; Shafi, Syed; Samim, Mohammed; Javed, Kalim; Supuran, Claudiu T (2023). Synthesis, biological evaluation and theoretical studies of (E)-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6366 DOI

Giovannuzzi, Simone; Bonardi, Alessandro; Gratteri, Paola; Nocentini, Alessio; Supuran, Claudiu T (2023). Discovery of the first-in-class potent and isoform-selective human carbonic anhydrase III inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6374 DOI

Astrain-Redin N.; Paoletti N.; Plano D.; Bonardi A.; Gratteri P.; Angeli A.; Sanmartin C.; Supuran C.T. (2023). Selenium-analogs based on natural sources as cancer-associated carbonic anhydrase isoforms IX and XII inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 2191165-2191165, ISSN:1475-6366 DOI Accesso ONLINE all'editore

Ragab, Mahmoud A; Eldehna, Wagdy M; Nocentini, Alessio; Bonardi, Alessandro; Okda, Hazem E; Elgendy, Bahaa; Ibrahim, Tarek S; Abd-Alhaseeb, Mohammad M; Gratteri, Paola; Supuran, Claudiu T; Al-Karmalawy, Ahmed A; Elagawany, Mohamed (2023). 4-(5-Amino-pyrazol-1-yl)benzenesulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and carbonic anhydrase: Design, synthesis, and biological assessments. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 250, pp. 115180-115180, ISSN:0223-5234 DOI

Badawi, Waleed A; Rashed, Mahmoud; Nocentini, Alessio; Bonardi, Alessandro; Abd-Alhaseeb, Mohammad M; Al-Rashood, Sara T; Veerakanellore, Giri Babu; Majrashi, Taghreed A; Elkaeed, Eslam B; Elgendy, Bahaa; Gratteri, Paola; Supuran, Claudiu T; Eldehna, Wagdy M; Elagawany, Mohamed (2023). Identification of new 4-(6-oxopyridazin-1-yl)benzenesulfonamides as multi-target anti-inflammatory agents targeting carbonic anhydrase, COX-2 and 5-LOX enzymes: synthesis, biological evaluations and modelling insights. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6374 DOI Accesso ONLINE all'editore

Abdoli, Morteza; Bonardi, Alessandro; Supuran, Claudiu T; Žalubovskis, Raivis (2023). 4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6366 DOI

Abdoli, Morteza; Bonardi, Alessandro; Supuran, Claudiu T; Žalubovskis, Raivis (2023). Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 38, pp. 0-0, ISSN:1475-6366 DOI

Ghouse, Shaik Mahammad; Sinha, Kareena; Bonardi, Alessandro; Pawar, Gaurav; Malasala, Satyaveni; Danaboina, Srikanth; Mohammed, Arifuddin; Yaddanapudi, Venkata M; Supuran, Claudiu T; Nanduri, Srinivas (2023). 6-Aminocoumarin oxime-ether/sulfonamides as selective hCA IX and XII inhibitors: Synthesis, evaluation, and molecular dynamics studies. ARCHIV DER PHARMAZIE, vol. 356, pp. 1-13, ISSN:1521-4184 DOI

Bonardi, Alessandro; Supuran, Claudiu T.; Nocentini, Alessio (2022). Phenols and Polyphenols as Carbonic Anhydrase Inhibitors. In: Alessandro Bonardi, Claudiu T Supuran, Alessio Nocentini. Phenols and Polyphenols as Carbonic Anhydrase Inhibitors, pp. 330-383 Bentham, ISBN:9789815079098. DOI

Aspatwar, Ashok; Barker, Harlan; Aisala, Heidi; Zueva, Ksenia; Kuuslahti, Marianne; Tolvanen, Martti; Primmer, Craig R; Lumme, Jaakko; Bonardi, Alessandro; Tripathi, Amit; Parkkila, Seppo; Supuran, Claudiu T (2022). Cloning, purification, kinetic and anion inhibition studies of a recombinant β-carbonic anhydrase from the Atlantic salmon parasite platyhelminth Gyrodactylus salaris. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 0-0, ISSN:1475-6366 DOI

Bonardi, Alessandro; Parkkila, Seppo; Supuran, Claudiu T (2022). Inhibition studies of the protozoan α-carbonic anhydrase from Trypanosoma cruzi with phenols. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 0-0, ISSN:1475-6366 DOI

Chiaramonte N.; Angeli A.; Sgambellone S.; Bonardi A.; Nocentini A.; Bartolucci G.; Braconi L.; Dei S.; Lucarini L.; Teodori E.; Gratteri P.; Wunsch B.; Supuran C.T.; Romanelli M.N. (2022). 2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 228, pp. 0-0, ISSN:0223-5234 DOI

Tawfik, Haytham O; Belal, Amany; Abourehab, Mohammed A S; Angeli, Andrea; Bonardi, Alessandro; Supuran, Claudiu T; El-Hamamsy, Mervat H (2022). Dependence on linkers' flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 0-0, ISSN:1475-6366 DOI

Banoglu, Erden; Ercanlı, Taner; Gür Maz, Tuğçe; Vullo, Daniela; Bonardi, Alessandro; Gratteri, Paola; Supuran, Claudiu T (2022). A Series of Thiadiazolyl-Benzenesulfonamides Incorporating an Aromatic Tail as Isoform-Selective, Potent Carbonic Anhydrase II/XII Inhibitors. CHEMMEDCHEM, vol. 17, pp. 0-0, ISSN:1860-7179 DOI

Bazzicalupi, Carla; Bonardi, Alessandro; Biver, Tarita; Ferraroni, Marta; Papi, Francesco; Savastano, Matteo; Lombardi, Paolo; Gratteri, Paola (2022). Probing the Efficiency of 13-Pyridylalkyl Berberine Derivatives to Human Telomeric G-Quadruplexes Binding: Spectroscopic, Solid State and In Silico Analysis. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 23, pp. 14061-14076, ISSN:1422-0067 DOI Accesso ONLINE all'editore

Al-Warhi, Tarfah; Elbadawi, Mostafa M; Bonardi, Alessandro; Nocentini, Alessio; Al-Karmalawy, Ahmed A; Aljaeed, Nada; Alotaibi, Ohoud J; Abdel-Aziz, Hatem A; Supuran, Claudiu T; Eldehna, Wagdy M (2022). Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 2635-2643, ISSN:1475-6374 DOI

Arias, Hugo R; Borghese, Cecilia M; Germann, Allison L; Pierce, Spencer R; Bonardi, Alessandro; Nocentini, Alessio; Gratteri, Paola; Thodati, Thanvi M; Lim, Natalie J; Harris, R Adron; Akk, Gustav (2022). (+)-Catharanthine potentiates the GABAA receptor by binding to a transmembrane site at the β(+)/α(-) interface near the TM2-TM3 loop. BIOCHEMICAL PHARMACOLOGY, vol. 199, pp. 114993-114993, ISSN:1873-2968 DOI

Bonardi, Alessandro; Micheli, Laura; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Gratteri, Paola; Nocentini, Alessio; Supuran, Claudiu T (2022). Development of Hydrogen Sulfide-Releasing Carbonic Anhydrases IX- and XII-Selective Inhibitors with Enhanced Antihyperalgesic Action in a Rat Model of Arthritis. JOURNAL OF MEDICINAL CHEMISTRY, vol. 65, pp. 13143-13157, ISSN:1520-4804 DOI

Onyılmaz, Mehmet; Koca, Murat; Bonardi, Alessandro; Degirmenci, Mustafa; Supuran, Claudiu T (2022). Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 743-748, ISSN:1475-6374 DOI

Nocentini A.; Bonardi A.; Pratesi S.; Gratteri P.; Dani C.; Supuran C.T. (2022). Pharmaceutical strategies for preventing toxicity and promoting antioxidant and anti-inflammatory actions of bilirubin. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 487-501, ISSN:1475-6366 DOI Accesso ONLINE all'editore

Sbravati D.; Bonardi A.; Bua S.; Angeli A.; Ferraroni M.; Nocentini A.; Casnati A.; Gratteri P.; Sansone F.; Supuran C.T. (2022). Calixarenes Incorporating Sulfonamide Moieties: Versatile Ligands for Carbonic Anhydrases Inhibition. CHEMISTRY-A EUROPEAN JOURNAL, vol. 28, pp. 1-8, ISSN:0947-6539 DOI Accesso ONLINE all'editore

Elimam D.M.; Eldehna W.M.; Salem R.; Bonardi A.; Nocentini A.; Al-Rashood S.T.; Elaasser M.M.; Gratteri P.; Supuran C.T.; Allam H.A. (2022). Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 228, pp. 114008-114019, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Kumar R.; Kumar A.; Ram S.; Angeli A.; Bonardi A.; Nocentini A.; Gratteri P.; Supuran C.T.; Sharma P.K. (2022). Novel benzenesulfonamide-bearing pyrazoles and 1,2,4-thiadiazoles as selective carbonic anhydrase inhibitors. ARCHIV DER PHARMAZIE, vol. 355, pp. e2100241-e2100241, ISSN:0365-6233 DOI Accesso ONLINE all'editore

Bonardi, Alessandro; Bua, Silvia; Combs, Jacob; Lomelino, Carrie; Andring, Jacob; Osman, Sameh Mohamed; Toti, Alessandra; Di Cesare Mannelli, Lorenzo; Gratteri, Paola; Ghelardini, Carla; McKenna, Robert; Nocentini, Alessio; Supuran, Claudiu T (2022). The three-tails approach as a new strategy to improve selectivity of action of sulphonamide inhibitors against tumour-associated carbonic anhydrase IX and XII. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 37, pp. 930-939-939, ISSN:1475-6366 DOI

Abdelrahman M.A.; Ibrahim H.S.; Nocentini A.; Eldehna W.M.; Bonardi A.; Abdel-Aziz H.A.; Gratteri P.; Abou-Seri S.M.; Supuran C.T. (2021). Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 209, pp. 0-0, ISSN:0223-5234 DOI

Bonardi A.; Nocentini A.; Osman S.M.; Alasmary F.A.; Almutairi T.M.; Abdullah D.S.; Gratteri P.; Supuran C.T. (2021). Inhibition of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with aromatic sulphonamides and clinically licenced drugs–a joint docking/molecular dynamics study. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 36, pp. 469-479, ISSN:1475-6366 DOI Accesso ONLINE all'editore

Eldeeb A.H.; Abo-Ashour M.F.; Angeli A.; Bonardi A.; Lasheen D.S.; Elrazaz E.Z.; Nocentini A.; Gratteri P.; Abdel-Aziz H.A.; Supuran C.T. (2021). Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 221, pp. 113486-113509, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Bonardi Alessandro (2021). In silico strategies for the rational design, synthesis, and biological evaluation of ligands targeting macromolecules of pharmaceutical interest. (Tutor: Paola Gratteri, Claudiu T. Supuran)

Grande R.; Carradori S.; Puca V.; Vitale I.; Angeli A.; Nocentini A.; Bonardi A.; Gratteri P.; Lanuti P.; Bologna G.; Simeone P.; Capasso C.; De Luca V.; Supuran C.T. (2021). Selective inhibition of helicobacter pylori carbonic anhydrases by carvacrol and thymol could impair biofilm production and the release of outer membrane vesicles. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 22, pp. 11583-11603, ISSN:1661-6596 DOI Accesso ONLINE all'editore

Elimam D.M.; Elgazar A.A.; Bonardi A.; Abdelfadil M.; Nocentini A.; El-Domany R.A.; Abdel-Aziz H.A.; Badria F.A.; Supuran C.T.; Eldehna W.M. (2021). Natural inspired piperine-based sulfonamides and carboxylic acids as carbonic anhydrase inhibitors: Design, synthesis and biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 225, pp. 113800--, ISSN:0223-5234 DOI

Lucarini E., Nocentini A., Bonardi A., Chiaramonte N., Parisio C., Micheli L., Toti A., Ferrara V., Carrino D., Pacini A., Romanelli M.N., Supuran C.T., Ghelardini C., Di Cesare Mannelli L. (2021). Carbonic Anhydrase IV Selective Inhibitors Counteract the Development of Colitis-Associated Visceral Pain in Rats. CELLS, vol. 10, pp. 2540-2555, ISSN:2073-4409 DOI

Guglielmi P.; Rotondi G.; Secci D.; Angeli A.; Chimenti P.; Nocentini A.; Bonardi A.; Gratteri P.; Carradori S.; Supuran C.T. (2020). Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 35, pp. 1891-1905, ISSN:1475-6366 DOI

Bonardi A.; Nocentini A.; Bua S.; Combs J.; Lomelino C.; Andring J.; Lucarini L.; Sgambellone S.; Masini E.; McKenna R.; Gratteri P.; Supuran C.T. (2020). Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action. JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, pp. 7422-7444, ISSN:0022-2623 DOI

Alkhaldi A.A.M.; Al-Sanea M.M.; Nocentini A.; Eldehna W.M.; Elsayed Z.M.; Bonardi A.; Abo-Ashour M.F.; El-Damasy A.K.; Abdel-Maksoud M.S.; Al-Warhi T.; Gratteri P.; Abdel-Aziz H.A.; Supuran C.T.; El-Haggar R. (2020). 3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 207, pp. 0-0, ISSN:0223-5234 DOI

Bonardi A.; Nocentini A.; Cadoni R.; Del Prete S.; Dumy P.; Capasso C.; Gratteri P.; Supuran C.T.; Winum J.-Y. (2020). Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium Vibrio cholerae. ACS MEDICINAL CHEMISTRY LETTERS, vol. 11, pp. 2277-2284, ISSN:1948-5875 DOI Accesso ONLINE all'editore

Clima L.; Craciun B.F.; Angeli A.; Petreni A.; Bonardi A.; Nocentini A.; Carta F.; Gratteri P.; Pinteala M.; Supuran C.T. (2020). Synthesis, Computational Studies and Assessment of in Vitro Activity of Squalene Derivatives as Carbonic Anhydrase Inhibitors. CHEMMEDCHEM, vol. 15, pp. 2052-2057, ISSN:1860-7179 DOI

Petreni A.; Bonardi A.; Lomelino C.; Osman S.M.; ALOthman Z.A.; Eldehna W.M.; El-Haggar R.; McKenna R.; Nocentini A.; Supuran C.T. (2020). Inclusion of a 5-fluorouracil moiety in nitrogenous bases derivatives as human carbonic anhydrase IX and XII inhibitors produced a targeted action against MDA-MB-231 and T47D breast cancer cells. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 190, pp. 112112--, ISSN:0223-5234 DOI

Said M.A.; Eldehna W.M.; Nocentini A.; Fahim S.H.; Bonardi A.; Elgazar A.A.; Krystof V.; Soliman D.H.; Abdel-Aziz H.A.; Gratteri P.; Abou-Seri S.M.; Supuran C.T. (2020). Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 189, pp. 1-14, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Pustenko A.; Nocentini A.; Gratteri P.; Bonardi A.; Vozny I.; Zalubovskis R.; Supuran C.T. (2020). The antibiotic furagin and its derivatives are isoform-selective human carbonic anhydrase inhibitors. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 35, pp. 1011-1020, ISSN:1475-6366 DOI

Said M.A.; Eldehna W.M.; Nocentini A.; Bonardi A.; Fahim S.H.; Bua S.; Soliman D.H.; Abdel-Aziz H.A.; Gratteri P.; Abou-Seri S.M.; Supuran C.T. (2020). Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 185, pp. 1-13, ISSN:0223-5234 DOI

Abdelrahman M.A.; Eldehna W.M.; Nocentini A.; Bua S.; Al-Rashood S.T.; Hassan G.S.; Bonardi A.; Almehizia A.A.; Alkahtani H.M.; Alharbi A.; Gratteri P.; Supuran C.T. (2019). Novel diamide-based benzenesulfonamides as selective carbonic anhydrase ix inhibitors endowed with antitumor activity: Synthesis, biological evaluation and in silico insights. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 20, pp. 2484-2499, ISSN:1661-6596 DOI Accesso ONLINE all'editore

Alessandro Bonardi, Paola Gratteri, Alessio Nocentini (2019). Chpater 19 Carbonic Anhydrases from Pathogens: Fungal Carbonic Anhydrases And Their Inhibitors as Potential Antifungal Agents.. In: C.T. Supuran, A. Nocentini. Carbonic Anhydrases, pp. 419-448 Elsevier, ISBN:978-0-12-816476-1. DOI Accesso ONLINE all'editore

Eldehna, Wagdy M.*; Abo-Ashour, Mahmoud F.; Nocentini, Alessio; El-Haggar, Radwan S.; Bua, Silvia; Bonardi, Alessandro; Al-Rashood, Sara T.; Hassan, Ghada S.; Gratteri, Paola; Abdel-Aziz, Hatem A.; Supuran, Claudiu T. (2019). Enhancement of the tail hydrophobic interactions within the carbonic anhydrase IX active site via structural extension: Design and synthesis of novel N-substituted isatins-SLC-0111 hybrids as carbonic anhydrase inhibitors and antitumor agents. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 162, pp. 147-160, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Bonardi, Alessandro; Vermelho, Alane Beatriz; Da Silva Cardoso, Veronica; De Souza Pereira, Mirian Claudia; Da Silva Lara, Leonardo; Selleri, Silvia; Gratteri, Paola; Supuran, Claudiu T.; Nocentini, Alessio (2019). N-Nitrosulfonamides as Carbonic Anhydrase Inhibitors: A Promising Chemotype for Targeting Chagas Disease and Leishmaniasis. ACS MEDICINAL CHEMISTRY LETTERS, vol. 10, pp. 413-418, ISSN:1948-5875 DOI Accesso ONLINE all'editore

Bonardi, Alessandro; Supuran, Claudiu T (2019). Treatment of glaucoma and ocular hypertension using rho kinase inhibitors: patent evaluation of US2018244666 and US2018256595. EXPERT OPINION ON THERAPEUTIC PATENTS, vol. 29, pp. 0-0, ISSN:1354-3776 DOI

Eldehna W.M.; Abdelrahman M.A.; Nocentini A.; Bua S.; Al-Rashood S.T.; Hassan G.S.; Bonardi A.; Almehizia A.A.; Alkahtani H.M.; Alharbi A.; Gratteri P.; Supuran C.T. (2019). Synthesis, biological evaluation and in silico studies with 4-benzylidene-2-phenyl-5(4H)-imidazolone-based benzenesulfonamides as novel selective carbonic anhydrase IX inhibitors endowed with anticancer activity. BIOORGANIC CHEMISTRY, vol. 90, pp. 103102-103111, ISSN:0045-2068 DOI Accesso ONLINE all'editore

Kalinin, Stanislav; Nocentini, Alessio; Kovalenko, Alexander; Sharoyko, Vladimir; Bonardi, Alessandro; Angeli, Andrea; Gratteri, Paola; Tennikova, Tatiana B.; Supuran, Claudiu T.; Krasavin, Mikhail (2019). From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 182, pp. 111642-111660, ISSN:1768-3254 DOI

Abo-Ashour M.F.; Eldehna W.M.; Nocentini A.; Bonardi A.; Bua S.; Ibrahim H.S.; Elaasser M.M.; Krystof V.; Jorda R.; Gratteri P.; Abou-Seri S.M.; Supuran C.T. (2019). 3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 184, pp. 1-11, ISSN:0223-5234 DOI

Niccolò Chiaramonte, Silvia Bua, Marta Ferraroni, Alessio Nocentini, Alessandro Bonardi, Gian Luca Bartolucci, Maria Concetta Durante, Laura Lucarini, Donata Chiapponi, Silvia Dei, Dina Manetti, Elisabetta Teodori, Paola Gratteri, Emanuela Masini, Claudiu T. Supuran, Maria Novella Romanelli (2018). 2-Benzylpiperazine: a new scaffold for potent human Carbonic Anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents.. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 151, pp. 363-375, ISSN:1768-3254 DOI

Bonardi, Alessandro; Falsini, Matteo; Catarzi, Daniela; Varano, Flavia; Di Cesare Mannelli, Lorenzo; Tenci, Barbara; Ghelardini, Carla; Angeli, Andrea; Supuran, Claudiu T.; Colotta, Vittoria* (2018). Structural investigations on coumarins leading to chromeno[4,3-c]pyrazol-4-ones and pyrano[4,3-c]pyrazol-4-ones: New scaffolds for the design of the tumor-associated carbonic anhydrase isoforms IX and XII. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 146, pp. 47-59, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Ibrahim, Hany S.*; Allam, Heba Abdelrasheed; Mahmoud, Walaa R.; Bonardi, Alessandro; Nocentini, Alessio; Gratteri, Paola; Ibrahim, Eslam S.; Abdel-Aziz, Hatem A.; Supuran, Claudiu T. (2018). Dual-tail arylsulfone-based benzenesulfonamides differently match the hydrophobic and hydrophilic halves of human carbonic anhydrases active sites: Selective inhibitors for the tumor-associated hCA IX isoform. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 152, pp. 1-9, ISSN:0223-5234 DOI Accesso ONLINE all'editore

Nocentini, Alessio; Bonardi, Alessandro; Gratteri, Paola; Cerra, Bruno; Gioiello, Antimo*; Supuran, Claudiu T. (2018). Steroids interfere with human carbonic anhydrase activity by using alternative binding mechanisms. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 33, pp. 1453-1459, ISSN:1475-6366 DOI Accesso ONLINE all'editore

Alessandro BONARDI

Biography

Born in Florence on 06/11/1991.

Degree in Pharmaceutical Chemistry and Technology (grade: 110): University of Florence, 2016.

Ph.D. cum laude in the Field of Drugs and Innovative Treatments (SSD CHEM-07/A), University of Florence, 2021.

Researcher (RTDA) at the University of Florence since 2022.

Alessandro BONARDI

Curriculum

EDUCATION

December 2016: Master’s Degree in Pharmaceutical Chemistry and Technology, University of Florence.

Thesis Title: "Structural investigation of coumarin derivatives for the development of new potent Carbonic Anhydrase IX and XII inhibitors".

Supervisor: Prof. Vittoria Colotta; Co-Supervisor: Prof. Flavia Varano.

Final Grade: 110/110.

November 2017 – October 2020: Ph.D. cum laude in the Field of Drugs and Innovative Treatments – Pharmaceutical Sciences Curriculum (XXXIII cycle). SSD CHEM-07/A.

Department of NEUROFARBA, University of Florence.

Thesis Title: "In silico strategies for the rational design, synthesis, and biological evaluation of ligands targeting macromolecules of pharmaceutical interest".

Supervisor: Prof. Paola Gratteri; Co-Supervisor: Prof. Claudiu T. Supuran.

January 2020 – March 2020: Ph.D. research period in Vienna at the research group of Prof. Vittorio Pace, Pharmaziezentrum, University of Vienna, Austria.

February 2021: Ph.D. degree awarded cum laude.

PROFESSIONAL EXPERIENCE

November 2020 – December 2022: Research Fellow at the Department of NEUROFARBA (Section of Pharmaceutical and Nutraceutical Sciences), University of Florence.

December 2022 – Present: University Researcher (RTDA) at the Department of NEUROFARBA (Section of Pharmaceutical and Nutraceutical Sciences), University of Florence.

SCIENTIFIC ACTIVITY

Dr. Bonardi (author of over 60 publications) has primarily focused his research on the in silico design, synthesis, and biological evaluation of modulators targeting pharmaceutical-relevant biological macromolecules, including enzymes, G-protein-coupled receptors (GPCRs), and nucleic acids.

His main research interests include: ▪ various aspects of Carbonic Anhydrase (CA) metalloenzymes as drug targets, covering in silico design, synthesis, and enzymatic kinetics evaluation using the Stopped-Flow technique to determine activation or inhibition profiles of CA modulators; ▪ in silico design and synthesis of ligands for Penicillin Binding Proteins (PBP), ribosomes, GABA_A ionotropic receptors, and GPCRs, such as β-adrenergic receptors; ▪ in silico studies, synthesis, and evaluation of ligand interactions with nucleic acids in both canonical (double-helix) and non-canonical (G-quadruplex) conformations.

Currently, Dr. Bonardi's research also extends to multi-target approaches for drug development, designing and synthesizing derivatives that merge CA inhibitory pharmacophores with active elements targeting other receptors. This approach is applied to: G-quadruplex intercalating ligands, antibacterial agents, anti-Alzheimer compounds, and selective β3-adrenergic receptor antagonists (where Structure-Based Virtual Screening has been used for hit compound identification).

TEACHING ACTIVITIES

From A.Y. 2021-2022 – Present: Lecturer for the Molecular Modeling in Pharmaceutical Chemistry course (3 CFU), an elective educational activity (EED) for Master’s Degree programs in LM13-Pharmacy, University of Florence.

From A.Y. 2021-2022 – Present: Lecturer for the Medicinal Analysis I – Module II course, LM13-Pharmacy, University of Florence.

From A.Y. 2023-2024 – Present: Lecturer for the Advanced Pharmaceutical Chemistry course, LM13-Pharmaceutical Chemistry and Technology, University of Florence.

Additionally, Dr. Bonardi is a member of the examination committees for the Medicinal and Toxicological Chemistry II course (LM13-Pharmacy), University of Florence.

Alessandro BONARDI

Interest

- Development of selective modulators for carbonic anhydrase isoforms.

- Development of multitarget compounds for the treatment of multifactorial diseases (e.g. glaucoma, cancer, Alzheimer’s disease, inflammatory diseases, infections, etc.).

- Evaluation of carbonic anhydrase modulator activity through enzymatic kinetics studies.

- In silico drug design (Virtual Screening, Docking, Molecular Dynamics, ADMET property prediction).

Alessandro BONARDI

Note

alessandro.bonardi@unifi.it