Research Topics
| Fulvio GualtieriSummaryAffiliation: University of Florence Country: Italy Publications
| Collaborators
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Detail Information
Publications
Design and study of piracetam-like nootropics, controversial members of the problematic class of cognition-enhancing drugsFulvio 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...- Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugsSerena 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... - 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 agonistSerena 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)... - Enantioselective synthesis and preliminary pharmacological evaluation of the enantiomers of unifiram (DM232), a potent cognition-enhancing agentElisabetta Martini
Dipartimento di Scienze Farmaceutiche, , 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... - Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic painElisabetta 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... - Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteinsDina 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... - 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 derivativesSilvia 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... - 4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugsDina Manetti
Dipartimento di Scienze Farmaceutiche, , 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... - Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitorsElisabetta 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... - 2-pyrrolidinone moiety is not critical for the cognition-enhancing activity of piracetam-like drugsSerena 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... - 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 iodomethylatesSilvia Dei
Dipartimento di Scienze Farmaceutiche, , 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... - Exploratory chemistry toward the identification of a new class of multidrug resistance reverters inspired by pervilleine and verapamil modelsElisabetta Teodori
Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
J Med Chem 48:7426-36. 2005.... - Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applicationsM 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... - A recombinant transductor-effector system: in vitro study of G inhibitory protein (G-alpha-i1) direct activatorsLorenzo 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... - Central nicotinic receptors: structure, function, ligands, and therapeutic potentialM 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.... - Sigma receptor binding profile of a series of analgesic tropane derivativesOrazio Prezzavento
Dipartimento di Scienze Framaceutiche, , 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...