Standard
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation. / Brogi, Simone; Brindisi, Marghertia; Butini, Stefania; Kshirsagar, Giridhar; Maramai, Samuele; Chemi, Giulia; Gemma, Sandra; Campiani, Giuseppe; Novellino, Ettore; Fiorenzani, Paolo; Pinassi, Jessica; Aloisi, Anna Maria; Gynther, Mikko; Venskutonyte, Raminta; Han, Liwei; Frydenvang, Karla Andrea; Kastrup, Jette Sandholm Jensen; Pickering, Darryl S.
In:
Journal of Medicinal Chemistry, Vol. 61, No. 5, 08.03.2018, p. 2124-2130.
Research output: Contribution to journal › Journal article › Research › peer-review
Harvard
Brogi, S, Brindisi, M, Butini, S, Kshirsagar, G, Maramai, S, Chemi, G, Gemma, S, Campiani, G, Novellino, E, Fiorenzani, P, Pinassi, J, Aloisi, AM, Gynther, M, Venskutonyte, R, Han, L
, Frydenvang, KA, Kastrup, JSJ & Pickering, DS 2018, '
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.',
Journal of Medicinal Chemistry, vol. 61, no. 5, pp. 2124-2130.
https://doi.org/10.1021/acs.jmedchem.8b00099APA
Brogi, S., Brindisi, M., Butini, S., Kshirsagar, G., Maramai, S., Chemi, G., Gemma, S., Campiani, G., Novellino, E., Fiorenzani, P., Pinassi, J., Aloisi, A. M., Gynther, M., Venskutonyte, R., Han, L.
, Frydenvang, K. A., Kastrup, J. S. J., & Pickering, D. S. (2018).
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation. Journal of Medicinal Chemistry,
61(5), 2124-2130.
https://doi.org/10.1021/acs.jmedchem.8b00099Vancouver
Brogi S, Brindisi M, Butini S, Kshirsagar G, Maramai S, Chemi G et al.
(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation. Journal of Medicinal Chemistry. 2018 Mar 8;61(5):2124-2130.
https://doi.org/10.1021/acs.jmedchem.8b00099Author
Brogi, Simone ; Brindisi, Marghertia ; Butini, Stefania ; Kshirsagar, Giridhar ; Maramai, Samuele ; Chemi, Giulia ; Gemma, Sandra ; Campiani, Giuseppe ; Novellino, Ettore ; Fiorenzani, Paolo ; Pinassi, Jessica ; Aloisi, Anna Maria ; Gynther, Mikko ; Venskutonyte, Raminta ; Han, Liwei ; Frydenvang, Karla Andrea ; Kastrup, Jette Sandholm Jensen ; Pickering, Darryl S. / (S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation. In: Journal of Medicinal Chemistry. 2018 ; Vol. 61, No. 5. pp. 2124-2130.
Bibtex
@article{71a01ea322054860b3e7c9dcd5644931,
title = "(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.",
abstract = "Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1 and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).",
author = "Simone Brogi and Marghertia Brindisi and Stefania Butini and Giridhar Kshirsagar and Samuele Maramai and Giulia Chemi and Sandra Gemma and Giuseppe Campiani and Ettore Novellino and Paolo Fiorenzani and Jessica Pinassi and Aloisi, {Anna Maria} and Mikko Gynther and Raminta Venskutonyte and Liwei Han and Frydenvang, {Karla Andrea} and Kastrup, {Jette Sandholm Jensen} and Pickering, {Darryl S}",
year = "2018",
month = mar,
day = "8",
doi = "10.1021/acs.jmedchem.8b00099",
language = "English",
volume = "61",
pages = "2124--2130",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "5",
}
RIS
TY - JOUR
T1 - (S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.
AU - Brogi, Simone
AU - Brindisi, Marghertia
AU - Butini, Stefania
AU - Kshirsagar, Giridhar
AU - Maramai, Samuele
AU - Chemi, Giulia
AU - Gemma, Sandra
AU - Campiani, Giuseppe
AU - Novellino, Ettore
AU - Fiorenzani, Paolo
AU - Pinassi, Jessica
AU - Aloisi, Anna Maria
AU - Gynther, Mikko
AU - Venskutonyte, Raminta
AU - Han, Liwei
AU - Frydenvang, Karla Andrea
AU - Kastrup, Jette Sandholm Jensen
AU - Pickering, Darryl S
PY - 2018/3/8
Y1 - 2018/3/8
N2 - Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1 and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).
AB - Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1 and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).
U2 - 10.1021/acs.jmedchem.8b00099
DO - 10.1021/acs.jmedchem.8b00099
M3 - Journal article
C2 - 29451794
VL - 61
SP - 2124
EP - 2130
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 5
ER -
