Fabrizio Carta

Summary

Affiliation: University of Florence
Country: Italy

Publications

  1. doi request reprint Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem 21:1564-9. 2013
  2. doi request reprint Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita degli Studi di Firenze, Rm 188 Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    J Med Chem 56:4691-700. 2013
  3. pmc Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita degli Studi di Firenze, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 55:1721-30. 2012
  4. doi request reprint New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 22:2182-5. 2012
  5. doi request reprint 5- and 6-membered (thio)lactones are prodrug type carbonic anhydrase inhibitors
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 22:267-70. 2012
  6. doi request reprint Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis
    Fabio Pacchiano
    Laboratorio di Chimica Bioinorganica, Rm 188, Polo Scientifico, Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 54:1896-902. 2011
  7. doi request reprint Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Florence, Italy
    Bioorg Med Chem 19:3105-19. 2011
  8. doi request reprint Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 17:7093-9. 2009
  9. doi request reprint Secondary and tertiary sulfonamides: a patent review (2008 - 2012)
    Andrea Scozzafava
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Expert Opin Ther Pat 23:203-13. 2013
  10. doi request reprint Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Chem Commun (Camb) 48:1868-70. 2012

Collaborators

Detail Information

Publications26

  1. doi request reprint Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem 21:1564-9. 2013
    ....
  2. doi request reprint Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita degli Studi di Firenze, Rm 188 Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    J Med Chem 56:4691-700. 2013
    ..Several xanthates showed potent intraocular pressure lowering activity in two animal models of glaucoma via the topical administration. Xanthates and thioxanthates represent two novel, promising classes of CA inhibitors...
  3. pmc Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Polo Scientifico, Universita degli Studi di Firenze, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 55:1721-30. 2012
    ..Some dithiocarbamates showed an effective intraocular pressure lowering activity in an animal model of glucoma...
  4. doi request reprint New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Florence, Italy
    Bioorg Med Chem Lett 22:2182-5. 2012
    ..This study demonstrates that a rather wide range of structures show low nanomolar-micromolar inhibitory activity against many CA isozymes, without inhibiting significantly the offtarget isoform CA II...
  5. doi request reprint 5- and 6-membered (thio)lactones are prodrug type carbonic anhydrase inhibitors
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 22:267-70. 2012
    ..Isoform-selective CA inhibitors which spare the ubiquitous off-target CA II may have interesting applications for example for selectively inhibiting the tumor-associated CA IX, a validated anticancer target...
  6. doi request reprint Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis
    Fabio Pacchiano
    Laboratorio di Chimica Bioinorganica, Rm 188, Polo Scientifico, Università degli Studi di Firenze, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 54:1896-902. 2011
    ....
  7. doi request reprint Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Florence, Italy
    Bioorg Med Chem 19:3105-19. 2011
    ..The 1,3,5-triazinyl-substituted benzenesulfonamides constitute thus a class of compounds with great potential for obtaining inhibitors targeting both α-class mammalian, tumor-associated, and β-class from pathogenic organisms CAs...
  8. doi request reprint Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the cytosolic isoforms I and II
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 17:7093-9. 2009
    ....
  9. doi request reprint Secondary and tertiary sulfonamides: a patent review (2008 - 2012)
    Andrea Scozzafava
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Expert Opin Ther Pat 23:203-13. 2013
    ..Many classes of compounds used in therapy present the substituted sulfonamide groups and there is also a continuous interest in different fields such as the herbicides herein schematically reported...
  10. doi request reprint Dithiocarbamates: a new class of carbonic anhydrase inhibitors. Crystallographic and kinetic investigations
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Chem Commun (Camb) 48:1868-70. 2012
    ..They coordinate to the zinc ion from the enzyme active site in monodentate manner and establish many favorable interactions with amino acid residues nearby. Several low nanomolar CA I, II and IX inhibitors were detected...
  11. doi request reprint Novel coumarins and 2-thioxo-coumarins as inhibitors of the tumor-associated carbonic anhydrases IX and XII
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem 20:2266-73. 2012
    ....
  12. doi request reprint Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, Rv3588c
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, I 50019 Sesto Fiorentino, Firenze, Italy
    Bioorg Med Chem Lett 19:6649-54. 2009
    ..As the Rv3588c gene was shown to be essential to the growth of M. tuberculosis, inhibition of this enzyme may be relevant for the design of antituberculosis drugs possessing a novel mechanism of action...
  13. doi request reprint Sulfonamides: a patent review (2008 - 2012)
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 22:747-58. 2012
    ..Recently, novel drugs have been launched, such as apricoxib and pazopanib, which also incorporate this group...
  14. doi request reprint Inhibition of β-carbonic anhydrases with ureido-substituted benzenesulfonamides
    Fabio Pacchiano
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Polo Scientifico, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 21:102-5. 2011
    ....
  15. doi request reprint Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem Lett 21:2521-6. 2011
    ..4-Hydroxy- and 4-methoxy-benzoate inhibited Can2 with K(I)s of 9.5-9.9 nM. The methyl esters, hydroxamates, hydrazides and carboxamides of some of these derivatives were also effective inhibitors of the α- and β-CAs investigated here...
  16. doi request reprint Carbonic anhydrase inhibitors: inhibition of cytosolic carbonic anhydrase isozymes II and VII with simple aromatic sulfonamides and some azo dyes
    Fabrizio Carta
    Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Sesto Fiorentino, Firenze, Italy
    Chem Biol Drug Des 74:196-202. 2009
    ..Good CA inhibitory activity was detected for some of these derivatives, with inhibition constants (Ki) in the range of 17.5-863 nm against CA II; and 30-4200 nm against CA VII...
  17. doi request reprint Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides
    Alfonso Maresca
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 19:4929-32. 2009
    ..Inhibition of pathogenic beta-CAs may lead to the development of antiinfectives with a new mechanism of action, devoid of resistance problems encountered with classical antibiotics...
  18. doi request reprint Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule
    Fabrizio Carta
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Florence, Italy
    J Med Chem 53:5511-22. 2010
    ..Spermine binds differently compared to sulfonamides, phenols, or coumarins, rendering possible to develop CAIs with a diverse inhibition mechanism, profile, and selectivity for various isoforms...
  19. doi request reprint Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors
    Murat Bozdag
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem Lett 23:715-9. 2013
    ..Herein we report the discovery of novel small-molecule, non peptidic PAD4 inhibitors incorporating primary/secondary guanidine moieties...
  20. doi request reprint Novel therapies for glaucoma: a patent review 2007 - 2011
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Expert Opin Ther Pat 22:79-88. 2012
    ..However, no new drugs have been launched on the market, although some new drug classes, such as 5-hydroxy-tryptamine (5HT(2)) agonists and rho kinase inhibitors entered into advanced clinical investigations...
  21. doi request reprint Antiglaucoma carbonic anhydrase inhibitors: a patent review
    Emanuela Masini
    Universita degli Studi di Firenze, NEUROFARBA Dept, Sezione di Farmacologia, Viale Pierracini 6, Florence, Italy
    Expert Opin Ther Pat 23:705-16. 2013
    ..2.1.1). CA inhibitors (CAIs) diminish intraocular pressure (IOP) by reducing the rate of bicarbonate formation and thus secretion of the aqueous humor...
  22. doi request reprint 7-Substituted-sulfocoumarins are isoform-selective, potent carbonic anhydrase II inhibitors
    Muhammet Tanc
    Universita degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, 50019 Sesto Fiorentino Florence, Italy
    Bioorg Med Chem 21:4502-10. 2013
    ..Since both hCA II and hCA VA are important drug targets (hCA II for antiglaucoma agents; hCA VA for antiobesity drugs), these isoform-selective inhibitors reported here may be considered of interest for various biomedical applications...
  23. doi request reprint Dithiocarbamates strongly inhibit the β-class carbonic anhydrases from Mycobacterium tuberculosis
    Alfonso Maresca
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino Florence, Italy
    J Enzyme Inhib Med Chem 28:407-11. 2013
    ....
  24. doi request reprint Antiobesity carbonic anhydrase inhibitors: a literature and patent review
    Andrea Scozzafava
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 23:725-35. 2013
    ..2.1.1) VA and VB as targets for the development of antiobesity drugs...
  25. doi request reprint Metalloenzyme inhibitors for the treatment of Gram-negative bacterial infections: a patent review (2009-2012)
    Claudiu T Supuran
    Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
    Expert Opin Ther Pat 23:777-88. 2013
    ..In particular, small molecules able to inhibit metalloenzymes are of interest for their use alone or in association with known antibiotics with the aim to reduce mutations and various drug resistance mechanisms...
  26. doi request reprint Diuretics with carbonic anhydrase inhibitory action: a patent and literature review (2005 - 2013)
    Fabrizio Carta
    Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
    Expert Opin Ther Pat 23:681-91. 2013
    ....