Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization

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Standard

Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists : Design, synthesis, and pharmacological characterization. / Conti, Paola; Pinto, Andrea; Tamborini, Lucia; Madsen, Ulf; Nielsen, Birgitte; Bräuner-Osborne, Hans; Hansen, Kasper Bø; Landucci, Elisa; Pellegrini-Giampietro, Domenico E; De Sarro, Giovambattista; Donato Di Paola, Eugenio; De Micheli, Carlo.

I: ChemMedChem, Bind 5, Nr. 9, 2010, s. 1465-1475.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Conti, P, Pinto, A, Tamborini, L, Madsen, U, Nielsen, B, Bräuner-Osborne, H, Hansen, KB, Landucci, E, Pellegrini-Giampietro, DE, De Sarro, G, Donato Di Paola, E & De Micheli, C 2010, 'Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization', ChemMedChem, bind 5, nr. 9, s. 1465-1475. https://doi.org/10.1002/cmdc.201000184

APA

Conti, P., Pinto, A., Tamborini, L., Madsen, U., Nielsen, B., Bräuner-Osborne, H., Hansen, K. B., Landucci, E., Pellegrini-Giampietro, D. E., De Sarro, G., Donato Di Paola, E., & De Micheli, C. (2010). Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization. ChemMedChem, 5(9), 1465-1475. https://doi.org/10.1002/cmdc.201000184

Vancouver

Conti P, Pinto A, Tamborini L, Madsen U, Nielsen B, Bräuner-Osborne H o.a. Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization. ChemMedChem. 2010;5(9):1465-1475. https://doi.org/10.1002/cmdc.201000184

Author

Conti, Paola ; Pinto, Andrea ; Tamborini, Lucia ; Madsen, Ulf ; Nielsen, Birgitte ; Bräuner-Osborne, Hans ; Hansen, Kasper Bø ; Landucci, Elisa ; Pellegrini-Giampietro, Domenico E ; De Sarro, Giovambattista ; Donato Di Paola, Eugenio ; De Micheli, Carlo. / Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists : Design, synthesis, and pharmacological characterization. I: ChemMedChem. 2010 ; Bind 5, Nr. 9. s. 1465-1475.

Bibtex

@article{259b5f00b4f911df825b000ea68e967b,
title = "Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: Design, synthesis, and pharmacological characterization",
abstract = "The design and synthesis of new N1-substituted 3-carboxy- and 3-phosphonopyrazoline and pyrazole amino acids that target the glutamate binding site of NMDA receptors are described. An analysis of the stereochemical requirements for high-affinity interaction with these receptors was performed. We identified two highly potent and selective competitive NMDA receptor antagonists, (5S,alphaR)-1 and (5S,alphaR)-4, which exhibit good in vitro neuroprotective activity and in vivo anticonvulsant activity by i.p. administration, suggesting that these molecules may have potential use as therapeutic agents.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Paola Conti and Andrea Pinto and Lucia Tamborini and Ulf Madsen and Birgitte Nielsen and Hans Br{\"a}uner-Osborne and Hansen, {Kasper B{\o}} and Elisa Landucci and Pellegrini-Giampietro, {Domenico E} and {De Sarro}, Giovambattista and {Donato Di Paola}, Eugenio and {De Micheli}, Carlo",
year = "2010",
doi = "10.1002/cmdc.201000184",
language = "English",
volume = "5",
pages = "1465--1475",
journal = "Farmaco",
issn = "1860-7179",
publisher = "Wiley - V C H Verlag GmbH & Co. KGaA",
number = "9",

}

RIS

TY - JOUR

T1 - Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists

T2 - Design, synthesis, and pharmacological characterization

AU - Conti, Paola

AU - Pinto, Andrea

AU - Tamborini, Lucia

AU - Madsen, Ulf

AU - Nielsen, Birgitte

AU - Bräuner-Osborne, Hans

AU - Hansen, Kasper Bø

AU - Landucci, Elisa

AU - Pellegrini-Giampietro, Domenico E

AU - De Sarro, Giovambattista

AU - Donato Di Paola, Eugenio

AU - De Micheli, Carlo

PY - 2010

Y1 - 2010

N2 - The design and synthesis of new N1-substituted 3-carboxy- and 3-phosphonopyrazoline and pyrazole amino acids that target the glutamate binding site of NMDA receptors are described. An analysis of the stereochemical requirements for high-affinity interaction with these receptors was performed. We identified two highly potent and selective competitive NMDA receptor antagonists, (5S,alphaR)-1 and (5S,alphaR)-4, which exhibit good in vitro neuroprotective activity and in vivo anticonvulsant activity by i.p. administration, suggesting that these molecules may have potential use as therapeutic agents.

AB - The design and synthesis of new N1-substituted 3-carboxy- and 3-phosphonopyrazoline and pyrazole amino acids that target the glutamate binding site of NMDA receptors are described. An analysis of the stereochemical requirements for high-affinity interaction with these receptors was performed. We identified two highly potent and selective competitive NMDA receptor antagonists, (5S,alphaR)-1 and (5S,alphaR)-4, which exhibit good in vitro neuroprotective activity and in vivo anticonvulsant activity by i.p. administration, suggesting that these molecules may have potential use as therapeutic agents.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1002/cmdc.201000184

DO - 10.1002/cmdc.201000184

M3 - Journal article

C2 - 20665761

VL - 5

SP - 1465

EP - 1475

JO - Farmaco

JF - Farmaco

SN - 1860-7179

IS - 9

ER -

ID: 21699538