![Fabrizio Pertusati](https://profiles-cardiff.imgix.net/attachments/2949?w=200&h=200&auto=format&crop=faces&fit=crop&q=90")
Dr Fabrizio Pertusati
Lecturer
- Ar gael fel goruchwyliwr ôl-raddedig
Trosolwyg
Cyhoeddiad
2023
- Serpi, M. et al. 2023. Synthesis, molecular docking and antibacterial activity of an oxadiazole-based lipoteichoic acid inhibitor and its metabolites. Journal of Molecular Structure 1278, article number: 134977. (10.1016/j.molstruc.2023.134977)
- Cook, S. R., Kirkham, E. D., Best, H., Waller-Evans, H., Serpi, M., Pertusati, F. and Lloyd-Evans, E. 2023. Investigating lysosomal and cellular phenotypes of the lysosomal disorder cystinosis. Presented at: 19th Annual WORLDSymposium™ 2023, Orlando, Florida, 21-26 February 2023, Vol. 138. Vol. 2. Elsevier pp. 28-28., (10.1016/j.ymgme.2022.107061)
2022
- Pertusati, F. and Morewood, J. 2022. Synthesis of 2‐Acetamido‐1,3,4‐Tri‐O‐Acetyl‐2‐Deoxy‐D‐Mannopyranose ‐6‐Phosphate Prodrugs as potential therapeutic agents. Current Protocols 2(8), article number: e500. (10.1002/cpz1.500)
2021
- Vanden Avond, M. A. et al. 2021. The nucleotide prodrug CERC‐913 improves mtDNA content in primary hepatocytes from DGUOK‐deficient rats. Journal of Inherited Metabolic Disease 44(2), pp. 492-501. (10.1002/jimd.12354)
- Serpi, M. and Pertusati, F. 2021. An overview of ProTide technology and its implications to drug discovery. Expert Opinion on Drug Discovery 16(10), pp. 1149--1161. (10.1080/17460441.2021.1922385)
2020
- Pertusati, F. et al. 2020. Drug repurposing: phosphate prodrugs of anticancer and antiviral FDA-approved nucleosides as novel antimicrobials. Journal of Antimicrobial Chemotherapy 75(10), pp. 2864-2878. (10.1093/jac/dkaa268)
2019
- Pertusati, F., Ferla, S., Bassetto, M., Brancale, A., Kandil, S., Westwell, A. D. and McGuigan, C. 2019. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer. European Journal of Medicinal Chemistry 180, pp. 1-14. (10.1016/j.ejmech.2019.07.001)
- Morozzi, C. et al. 2019. Targeting GNE myopathy: A dual prodrug approach for the delivery of N-acetylmannosamine 6-phosphate. Journal of Medicinal Chemistry 62(17), pp. 8178-8193. (10.1021/acs.jmedchem.9b00833)
2018
- Pileggi, E., Serpi, M. and Pertusati, F. 2018. Preparation of pyrimidine alkenyl acyclic nucleoside phosphonoamidates. Current Protocols in Nucleic Acid Chemistry 74(13-14), article number: e56. (10.1002/cpnc.56)
- Pileggi, E., Serpi, M., Andrei, G., Schols, D., Snoeck, R. and Pertusati, F. 2018. Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs. Bioorganic and Medicinal Chemistry 26(12), pp. 3596-3609. (10.1016/j.bmc.2018.05.034)
- Slusarczyk, M., Serpi, M. and Pertusati, F. 2018. Phosphoramidates and phosphonamidates (ProTides) with antiviral activity. Antiviral Chemistry and Chemotherapy 26, pp. 1-31. (10.1177/2040206618775243)
2017
- Pertusati, F., Serafini, S., Albadry, N., Snoeck, R. and Andrei, G. 2017. Phosphonoamidate prodrugs of C5-substituted pyrimidine acyclic nucleosides for antiviral therapy. Antiviral Research 143, pp. 262-268. (10.1016/j.antiviral.2017.04.013)
- Serpi, M., De Biasi, R., Pertusati, F., Slusarczyk, M. and McGuigan, C. 2017. Synthetic approaches for the preparation of phosphoramidate prodrugs of 2’-deoxypseudoisocytidine. ChemistryOpen 6(3), pp. 424-436. (10.1002/open.201700019)
- Bassetto, M., Ferla, S., Giancotti, G., Pertusati, F., Westwell, A. D., Brancale, A. and McGuigan, C. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8(7), pp. 1414-1420. (10.1039/C7MD00164A)
- James, E., Pertusati, F., Brancale, A. and McGuigan, C. 2017. Kinase-independent phosphoramidate S1P1 receptor agonist benzyl ether derivatives. Biorganic and Medicinal Chemistry Letters 27(6), pp. 1371-1378. (10.1016/j.bmcl.2017.02.011)
- Pertusati, F., Nutz, E., Kariuki, B. and Coogan, M. P. 2017. Synthesis and substrate-controlled reactions of 2,2′-unsaturated biquinazolinones. Tetrahedron 73(1), pp. 55-63. (10.1016/j.tet.2016.11.060)
2016
- Marinozzi, M., Pertusati, F. and Serpi, M. 2016. λ5-Phosphorus-Containing α-Diazo Compounds (PCDCs): a valuable tool for accessing phosphorus-functionalized molecules. Chemical Reviews 116(22), pp. 13991-14055. (10.1021/acs.chemrev.6b00373)
- Serpi, M., Ferrari, V. and Pertusati, F. 2016. Nucleosided derived antibiotics to fight microbial drug resistance: New utilities for an established class of drugs?. Journal of Medicinal Chemistry 59(23), pp. 10343-10382. (10.1021/acs.jmedchem.6b00325)
- Bassetto, M., Ferla, S., Pertusati, F., Kandil, S., Westwell, A., Brancale, A. and McGuigan, C. 2016. Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. European Journal of Medicinal Chemistry 118, pp. 230-243. (10.1016/j.ejmech.2016.04.052)
- Ferla, S., Bassetto, M., Pertusati, F., Kandil, S., Westwell, A. D., Brancale, A. and McGuigan, C. 2016. Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. Bioorganic and Medicinal Chemistry Letters 26(15), pp. 3636-3640. (10.1016/j.bmcl.2016.06.001)
- McGuigan, C. et al. 2016. Anti-flavivirus activity of different tritylated pyrimidine and purine nucleoside analogues. ChemistryOpen 5(3), pp. 227-235. (10.1002/open.201500216)
2015
- Pertusati, F. and McGuigan, C. 2015. Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction. Chemical Communications 51(38), pp. 8070-8073. (10.1039/C5CC00448A)
- Pertusati, F., McGuigan, C. and Serpi, M. 2015. Symmetrical diamidate prodrugs of nucleotide analogues for drug delivery. In: Current Protocols in Nucleic Acid Chemistry. Wiley-Blackwell, pp. 60:15.6.1-15.6.10., (10.1002/0471142700.nc1506s60)
- Ferrari, V., Serpi, M., McGuigan, C. and Pertusati, F. 2015. Chemoselective N-deacetylation of protected nucleosides and nucleotides promoted by the Schwartz's reagent. Nucleosides, Nucleotides & Nucleic Acids 34(11), pp. 799-814. (10.1080/15257770.2015.1075552)
2014
- Toti, K. S. et al. 2014. Synthesis of an apionucleoside family and discovery of a prodrug with anti-HIV activity. Journal of Organic Chemistry 79(11), pp. 5097-5112. (10.1021/jo500659e)
- Pertusati, F., Hinsinger, K., Flynn, ?. S., Powell, N. G., Tristram, A. J., Balzarini, J. and McGuigan, C. 2014. PMPA and PMEA prodrugs for the treatment of HIV infections and human papillomavirus (HPV) associated neoplasia and cancer. European Journal of Medicinal Chemistry 78, pp. 259-268. (10.1016/j.ejmech.2014.03.051)
- McGuigan, C. et al. 2014. ProTides of N-(3-(5-(2'-deoxyuridine))prop-2-ynyl)octanamide as potential anti-tubercular and anti-viral agents. Bioorganic and Medicinal Chemistry 22(9), pp. 2816-2824. (10.1016/j.bmc.2014.02.056)
2013
- McGuigan, C. et al. 2013. Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides. European Journal of Medicinal Chemistry 70, pp. 326-340. (10.1016/j.ejmech.2013.09.047)
2011
- Pertusati, F., Serpi, M. and McGuigan, C. 2011. Medicinal chemistry of nucleoside phosphonate prodrugs for antiviral therapy. Antiviral Chemistry and Chemotherapy 22(5), pp. 181-203. (10.3851/IMP2012)
2007
- Pertusati, F. 2007. Synthesis of atropisomeric 2,2'-disubstituted-3,3'-quinazolin-4,4'-diones and their application in asymmetric synthesis. PhD Thesis, Cardiff University.
Adrannau llyfrau
- Pertusati, F., McGuigan, C. and Serpi, M. 2015. Symmetrical diamidate prodrugs of nucleotide analogues for drug delivery. In: Current Protocols in Nucleic Acid Chemistry. Wiley-Blackwell, pp. 60:15.6.1-15.6.10., (10.1002/0471142700.nc1506s60)
Cynadleddau
- Cook, S. R., Kirkham, E. D., Best, H., Waller-Evans, H., Serpi, M., Pertusati, F. and Lloyd-Evans, E. 2023. Investigating lysosomal and cellular phenotypes of the lysosomal disorder cystinosis. Presented at: 19th Annual WORLDSymposium™ 2023, Orlando, Florida, 21-26 February 2023, Vol. 138. Vol. 2. Elsevier pp. 28-28., (10.1016/j.ymgme.2022.107061)
Erthyglau
- Serpi, M. et al. 2023. Synthesis, molecular docking and antibacterial activity of an oxadiazole-based lipoteichoic acid inhibitor and its metabolites. Journal of Molecular Structure 1278, article number: 134977. (10.1016/j.molstruc.2023.134977)
- Pertusati, F. and Morewood, J. 2022. Synthesis of 2‐Acetamido‐1,3,4‐Tri‐O‐Acetyl‐2‐Deoxy‐D‐Mannopyranose ‐6‐Phosphate Prodrugs as potential therapeutic agents. Current Protocols 2(8), article number: e500. (10.1002/cpz1.500)
- Vanden Avond, M. A. et al. 2021. The nucleotide prodrug CERC‐913 improves mtDNA content in primary hepatocytes from DGUOK‐deficient rats. Journal of Inherited Metabolic Disease 44(2), pp. 492-501. (10.1002/jimd.12354)
- Serpi, M. and Pertusati, F. 2021. An overview of ProTide technology and its implications to drug discovery. Expert Opinion on Drug Discovery 16(10), pp. 1149--1161. (10.1080/17460441.2021.1922385)
- Pertusati, F. et al. 2020. Drug repurposing: phosphate prodrugs of anticancer and antiviral FDA-approved nucleosides as novel antimicrobials. Journal of Antimicrobial Chemotherapy 75(10), pp. 2864-2878. (10.1093/jac/dkaa268)
- Pertusati, F., Ferla, S., Bassetto, M., Brancale, A., Kandil, S., Westwell, A. D. and McGuigan, C. 2019. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer. European Journal of Medicinal Chemistry 180, pp. 1-14. (10.1016/j.ejmech.2019.07.001)
- Morozzi, C. et al. 2019. Targeting GNE myopathy: A dual prodrug approach for the delivery of N-acetylmannosamine 6-phosphate. Journal of Medicinal Chemistry 62(17), pp. 8178-8193. (10.1021/acs.jmedchem.9b00833)
- Pileggi, E., Serpi, M. and Pertusati, F. 2018. Preparation of pyrimidine alkenyl acyclic nucleoside phosphonoamidates. Current Protocols in Nucleic Acid Chemistry 74(13-14), article number: e56. (10.1002/cpnc.56)
- Pileggi, E., Serpi, M., Andrei, G., Schols, D., Snoeck, R. and Pertusati, F. 2018. Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs. Bioorganic and Medicinal Chemistry 26(12), pp. 3596-3609. (10.1016/j.bmc.2018.05.034)
- Slusarczyk, M., Serpi, M. and Pertusati, F. 2018. Phosphoramidates and phosphonamidates (ProTides) with antiviral activity. Antiviral Chemistry and Chemotherapy 26, pp. 1-31. (10.1177/2040206618775243)
- Pertusati, F., Serafini, S., Albadry, N., Snoeck, R. and Andrei, G. 2017. Phosphonoamidate prodrugs of C5-substituted pyrimidine acyclic nucleosides for antiviral therapy. Antiviral Research 143, pp. 262-268. (10.1016/j.antiviral.2017.04.013)
- Serpi, M., De Biasi, R., Pertusati, F., Slusarczyk, M. and McGuigan, C. 2017. Synthetic approaches for the preparation of phosphoramidate prodrugs of 2’-deoxypseudoisocytidine. ChemistryOpen 6(3), pp. 424-436. (10.1002/open.201700019)
- Bassetto, M., Ferla, S., Giancotti, G., Pertusati, F., Westwell, A. D., Brancale, A. and McGuigan, C. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8(7), pp. 1414-1420. (10.1039/C7MD00164A)
- James, E., Pertusati, F., Brancale, A. and McGuigan, C. 2017. Kinase-independent phosphoramidate S1P1 receptor agonist benzyl ether derivatives. Biorganic and Medicinal Chemistry Letters 27(6), pp. 1371-1378. (10.1016/j.bmcl.2017.02.011)
- Pertusati, F., Nutz, E., Kariuki, B. and Coogan, M. P. 2017. Synthesis and substrate-controlled reactions of 2,2′-unsaturated biquinazolinones. Tetrahedron 73(1), pp. 55-63. (10.1016/j.tet.2016.11.060)
- Marinozzi, M., Pertusati, F. and Serpi, M. 2016. λ5-Phosphorus-Containing α-Diazo Compounds (PCDCs): a valuable tool for accessing phosphorus-functionalized molecules. Chemical Reviews 116(22), pp. 13991-14055. (10.1021/acs.chemrev.6b00373)
- Serpi, M., Ferrari, V. and Pertusati, F. 2016. Nucleosided derived antibiotics to fight microbial drug resistance: New utilities for an established class of drugs?. Journal of Medicinal Chemistry 59(23), pp. 10343-10382. (10.1021/acs.jmedchem.6b00325)
- Bassetto, M., Ferla, S., Pertusati, F., Kandil, S., Westwell, A., Brancale, A. and McGuigan, C. 2016. Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. European Journal of Medicinal Chemistry 118, pp. 230-243. (10.1016/j.ejmech.2016.04.052)
- Ferla, S., Bassetto, M., Pertusati, F., Kandil, S., Westwell, A. D., Brancale, A. and McGuigan, C. 2016. Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. Bioorganic and Medicinal Chemistry Letters 26(15), pp. 3636-3640. (10.1016/j.bmcl.2016.06.001)
- McGuigan, C. et al. 2016. Anti-flavivirus activity of different tritylated pyrimidine and purine nucleoside analogues. ChemistryOpen 5(3), pp. 227-235. (10.1002/open.201500216)
- Pertusati, F. and McGuigan, C. 2015. Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction. Chemical Communications 51(38), pp. 8070-8073. (10.1039/C5CC00448A)
- Ferrari, V., Serpi, M., McGuigan, C. and Pertusati, F. 2015. Chemoselective N-deacetylation of protected nucleosides and nucleotides promoted by the Schwartz's reagent. Nucleosides, Nucleotides & Nucleic Acids 34(11), pp. 799-814. (10.1080/15257770.2015.1075552)
- Toti, K. S. et al. 2014. Synthesis of an apionucleoside family and discovery of a prodrug with anti-HIV activity. Journal of Organic Chemistry 79(11), pp. 5097-5112. (10.1021/jo500659e)
- Pertusati, F., Hinsinger, K., Flynn, ?. S., Powell, N. G., Tristram, A. J., Balzarini, J. and McGuigan, C. 2014. PMPA and PMEA prodrugs for the treatment of HIV infections and human papillomavirus (HPV) associated neoplasia and cancer. European Journal of Medicinal Chemistry 78, pp. 259-268. (10.1016/j.ejmech.2014.03.051)
- McGuigan, C. et al. 2014. ProTides of N-(3-(5-(2'-deoxyuridine))prop-2-ynyl)octanamide as potential anti-tubercular and anti-viral agents. Bioorganic and Medicinal Chemistry 22(9), pp. 2816-2824. (10.1016/j.bmc.2014.02.056)
- McGuigan, C. et al. 2013. Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides. European Journal of Medicinal Chemistry 70, pp. 326-340. (10.1016/j.ejmech.2013.09.047)
- Pertusati, F., Serpi, M. and McGuigan, C. 2011. Medicinal chemistry of nucleoside phosphonate prodrugs for antiviral therapy. Antiviral Chemistry and Chemotherapy 22(5), pp. 181-203. (10.3851/IMP2012)
Gosodiad
- Pertusati, F. 2007. Synthesis of atropisomeric 2,2'-disubstituted-3,3'-quinazolin-4,4'-diones and their application in asymmetric synthesis. PhD Thesis, Cardiff University.
Ymchwil
The research in the group is mainly in synthetic organic chemistry aimed to solve a range of medicinal chemistry problems in the area of:
Rare Diseases
- Lysosomal Storage diseases: cystinosys, Nieman-Pick, Mucolipidoses IV.
Inborn errors of metabolism
- Synthesis of carbohydrate based compounds for the treatment of congenital disorder of glycosylation.
- Nucleoside derivative for the treatment of Mitocondrial Depletion Syndrome.
Infectious diseases
- Synthesis of nucleosides and non nucleoside scaffolds as novel antibacterial agents.
- Fluorinated heterocycles as anti-biofilm and antimicrobial agents.
- Fluorinated small molecules as novel antileishmaniasys drugs.
Synthetic Chemistry
-Synthesis of new acyclic nucleoside phosphate and phosphonate scaffolds as antiviral, anticancer and antibacterial drugs.
-Development of synthetic methodologies for the diasteroselective and enantioselective preparation of organophosphorus compounds via P(V) and P(III) chemistries.
Collaborators
Rare Diseases:
- Dr Emyr Lloyd Evans (Lysosomal storage disease, School of Bioscience)
- Professor Hudson Freeze (Congenital Disorder of Glycosylation, Sanford Burnham Institute, California)
- Professor Michael W. Lawlor (Mitochondrial Depletion Syndrome, Medical College of Wisconsin)
Infectious diseases
Antibacterial and antibiofilm.
- Professor Hans Steenhackers ( Centre of Microbial and Plant Genetics, KU Leuven)
- Professor David Williams (Cardiff School of Denstistry)
- Professor Marçal Pastor Anglada (University of Barcelona)
Addysgu
PH1125: Chemical and Biological Properties of Drug Molecules ( Module leader)
PH2114: Principles of Drug Design and Drug Disposition
PH3101: Optimisation of Drug Design
PH4116: Pharmacy Research or Scholarship Project
At the Cardiff School of Chemistry (2018-2020):
- CH0003 Chemistry of organic compounds
- CH4207 Intoduction to the chemistry of life
- CHT354 Drug Development from Laboratory to Clinic
- CHT216 Colloquium
Bywgraffiad
I obtained my MSc degree in physical organic chemistry from Turin University (synthesis and characterisation of cationic surfactants). After three years spent in PCB industry as formulator scientist, I obtained my PhD in synthetic organic chemistry (Cardiff School of Chemistry, atropisomeric bis-quinazolinones as chiral auxiliaries for asymmetric synthesis). I conducted my post-doctoral training at Emory University (solid-phase synthesis of polymethine dyes) and in the laboratory of the Nobel laureate Prof. George Olah, at the University of Southern California (organofluorine, organoboron and polymer chemistry).
Since 2011, I have been working in Chris McGuigan’s group where I was involved in various medicinal chemistry projects spanning from diastereoselective synthesis of nucleosides (cyclic and acyclic) phosphoroamidate prodrugs, to fluorinated androgen-receptors antagonist for prostate cancer treatment, and design and synthesis of novel compounds acting on the Central Nervous System).
In 2016, I was promoted to Research Fellow in medicinal chemistry. My current research interests are in the synthesis of novel fluorinated antibiotics for the treatment of Gram-positive bacterial infections and biofilm formation (in collaboration with prof. Hans Steenackers at Leuven University) and in congenital disorders of glycosylation. I am also interested in drug design for the treatment of lysosomal storage disorders (Niemann-Pick, Huntington) in collaboration with Dr. Lloyd-Evans (Cardiff School of Bioscience).
Aelodaethau proffesiynol
- Member of Scientific Advisory Board of Ichorion Therapeutics (2017-2018)
- Member of Glycobiology Society
Pwyllgorau ac adolygu
- Reviewer for The following Journal.
Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, The journal of Organic Chemistry, ChemMedChem, Molecules, Bioorganic & Medicinal Chemistry Letters, Journal of Fluorine Chemistry, Organic Letters and Dyes and Pigments.
- Grant Reviewer: MRC-fellowship.
