1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators

Stefania Butini; Darryl S Pickering; Elena Morelli; Salvatore Sanna Coccone; Francesco Trotta; Meri De Angelis; Egeria Guarino; Isabella Fiorini; Giuseppe Campiani; Ettore Novellino; Arne Schousboe; Jeppe K Christensen; Sandra Gemma

doi:10.1021/jm800865a

1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators

Stefania Butini, Darryl S Pickering, Elena Morelli, Salvatore Sanna Coccone, Francesco Trotta, Meri De Angelis, Egeria Guarino, Isabella Fiorini, Giuseppe Campiani, Ettore Novellino, Arne Schousboe, Jeppe K Christensen, Sandra Gemma

19 Citations (Scopus)

Abstract

(S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new potent, subunit selective iGluR5 modulators.

Original language	English
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	20
Pages (from-to)	6614-8
ISSN	0022-2623
DOIs	https://doi.org/10.1021/jm800865a
Publication status	Published - 2008

Keywords

Former Faculty of Pharmaceutical Sciences

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Butini, S., Pickering, D. S., Morelli, E., Coccone, S. S., Trotta, F., De Angelis, M., Guarino, E., Fiorini, I., Campiani, G., Novellino, E., Schousboe, A., Christensen, J. K., & Gemma, S. (2008). 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators. Journal of Medicinal Chemistry, 51(20), 6614-8. https://doi.org/10.1021/jm800865a

1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators. / Butini, Stefania; Pickering, Darryl S; Morelli, Elena et al.

In: Journal of Medicinal Chemistry, Vol. 51, No. 20, 2008, p. 6614-8.

Research output: Contribution to journal › Journal article › Research › peer-review

Butini, S, Pickering, DS, Morelli, E, Coccone, SS, Trotta, F, De Angelis, M, Guarino, E, Fiorini, I, Campiani, G, Novellino, E, Schousboe, A, Christensen, JK & Gemma, S 2008, '1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators', Journal of Medicinal Chemistry, vol. 51, no. 20, pp. 6614-8. https://doi.org/10.1021/jm800865a

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title = "1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators",

abstract = "(S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new potent, subunit selective iGluR5 modulators.",

keywords = "Former Faculty of Pharmaceutical Sciences",

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doi = "10.1021/jm800865a",

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T1 - 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators

AU - Butini, Stefania

AU - Pickering, Darryl S

AU - Morelli, Elena

AU - Coccone, Salvatore Sanna

AU - Trotta, Francesco

AU - De Angelis, Meri

AU - Guarino, Egeria

AU - Fiorini, Isabella

AU - Campiani, Giuseppe

AU - Novellino, Ettore

AU - Schousboe, Arne

AU - Christensen, Jeppe K

AU - Gemma, Sandra

PY - 2008

Y1 - 2008

N2 - (S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new potent, subunit selective iGluR5 modulators.

AB - (S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new potent, subunit selective iGluR5 modulators.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.1021/jm800865a

DO - 10.1021/jm800865a

M3 - Journal article

C2 - 18811139

SN - 0022-2623

VL - 51

SP - 6614

EP - 6618

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 20

ER -

1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. Structure-activity relationships and identification of potent and selective iGluR5 modulators

Abstract

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