Fulvio Gualtieri

Summary

Affiliation: University of Florence
Country: Italy

Publications

  1. ncbi request reprint Design and study of piracetam-like nootropics, controversial members of the problematic class of cognition-enhancing drugs
    Fulvio Gualtieri
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Curr Pharm Des 8:125-38. 2002
  2. ncbi request reprint Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem 12:71-85. 2004
  3. ncbi request reprint Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 49:1925-31. 2006
  4. ncbi request reprint Enantioselective synthesis and preliminary pharmacological evaluation of the enantiomers of unifiram (DM232), a potent cognition-enhancing agent
    Elisabetta Martini
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino FI, Italy
    Med Chem 1:473-80. 2005
  5. ncbi request reprint Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 47:6070-81. 2004
  6. ncbi request reprint Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteins
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, I 50019 Sesto Fiorentino FI, Italy
    J Med Chem 48:6491-503. 2005
  7. ncbi request reprint Muscarinic subtype affinity and functional activity profile of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)pyrrolidine and 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine derivatives
    Silvia Dei
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    Biochem Pharmacol 69:1637-45. 2005
  8. ncbi request reprint 4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem Lett 13:2303-6. 2003
  9. ncbi request reprint Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 50:599-602. 2007
  10. ncbi request reprint 2-pyrrolidinone moiety is not critical for the cognition-enhancing activity of piracetam-like drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121 Firenze, Italy
    Farmaco 58:715-22. 2003

Detail Information

Publications16

  1. ncbi request reprint Design and study of piracetam-like nootropics, controversial members of the problematic class of cognition-enhancing drugs
    Fulvio Gualtieri
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Curr Pharm Des 8:125-38. 2002
    ..Recent developments which hopefully will lead to a revival of the class are reviewed...
  2. ncbi request reprint Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem 12:71-85. 2004
    ..Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg...
  3. ncbi request reprint Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 49:1925-31. 2006
    ..65, alpha=0.41) while being a poor antagonist on M1, M3, and M4 model tissues (pKb<5)...
  4. ncbi request reprint Enantioselective synthesis and preliminary pharmacological evaluation of the enantiomers of unifiram (DM232), a potent cognition-enhancing agent
    Elisabetta Martini
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino FI, Italy
    Med Chem 1:473-80. 2005
    ..On the contrary, (R)-(+) and (S)-(-)-(2) showed the same amnesic potency when tested in the passive-avoidance test. These findings may be useful to clarify the mechanism of action of these substances...
  5. ncbi request reprint Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 47:6070-81. 2004
    ..Two compounds that show N-type calcium channel antagonism and are endowed with potent action on pain and neuropathic pain (3 and 18) have been selected for further studies...
  6. ncbi request reprint Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteins
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, I 50019 Sesto Fiorentino FI, Italy
    J Med Chem 48:6491-503. 2005
    ..Some of the compounds synthesized and found to be active may be useful leads to develop more potent and selective Gi protein modulators...
  7. ncbi request reprint Muscarinic subtype affinity and functional activity profile of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)pyrrolidine and 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine derivatives
    Silvia Dei
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    Biochem Pharmacol 69:1637-45. 2005
    ..Our results confirm that sterical complication of parent compounds (+)-1 and (+)-2 produces more selective muscarinic agonists...
  8. ncbi request reprint 4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem Lett 13:2303-6. 2003
    ..One of the new compounds (9, active at 0.01 mg/kg ip) may represent a new lead for the development of cognition enhancers useful to treat the cognitive deficit produced by neurodegenerative pathologies like Alzheimer's disease...
  9. ncbi request reprint Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 50:599-602. 2007
    ..Among them, compound 1d, on anthracycline-resistant erythroleukemia K562 cells, is able to completely reverse Pgp-dependent MDR at low nanomolar concentration...
  10. ncbi request reprint 2-pyrrolidinone moiety is not critical for the cognition-enhancing activity of piracetam-like drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121 Firenze, Italy
    Farmaco 58:715-22. 2003
    ..As found previously in the case of 1,4-diazabicyclo[4.3.0]nonan-9-one compounds, the cognition-enhancing activity of 2-pyrrolidinone compounds is maintained in most cases, suggesting that this moiety is not crucial for activity...
  11. ncbi request reprint Synthesis and cholinergic affinity of diastereomeric and enantiomeric isomers of 1-methyl-2-(2-methyl-1,3-dioxolan-4-yl)- pyrrolidine, 1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine and of Their iodomethylates
    Silvia Dei
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Gino Capponi 9, 50121 Firenze, Italy
    Bioorg Med Chem 11:3153-64. 2003
    ..While none of the compounds showed any nicotinic affinity up to the dose of 10 microM, most of the iodomethylates were endowed with promising affinity for the muscarinic receptors...
  12. ncbi request reprint Exploratory chemistry toward the identification of a new class of multidrug resistance reverters inspired by pervilleine and verapamil models
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 48:7426-36. 2005
    ....
  13. ncbi request reprint Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applications
    M Novella Romanelli
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Gino Capponi 9, 50121 Firenze, Italy
    Med Res Rev 23:393-426. 2003
    ..This review focuses on the structure of new ligands for nAChRs, agonists, antagonists and allosteric modulators, and on their possible applications...
  14. ncbi request reprint A recombinant transductor-effector system: in vitro study of G inhibitory protein (G-alpha-i1) direct activators
    Lorenzo Di Cesare Mannelli
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50134 Florence, Italy
    Arch Biochem Biophys 453:151-60. 2006
    ..In this functional transductor-effector system BC5 was able to activate Gi signalling, moreover providing a new tool to give a better insight into G-protein receptor-independent modulation...
  15. ncbi request reprint Central nicotinic receptors: structure, function, ligands, and therapeutic potential
    M Novella Romanelli
    Laboratory of Design, Synthesis, and Study of Biologically Active Heterocycles HeteroBioLab, Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    ChemMedChem 2:746-67. 2007
    ....
  16. ncbi request reprint Sigma receptor binding profile of a series of analgesic tropane derivatives
    Orazio Prezzavento
    Dipartimento di Scienze Framaceutiche, Universita di Firenze, Firenze, Italy
    Arch Pharm (Weinheim) 335:39-43. 2002
    ..Structure-affinity relationships for sigma receptor subtypes are discussed. They lead to the identification of a few useful leads for further development of potent sigma ligands within the series...