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( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
Brogi, Simone; Brindisi, Margherita; Butini, Stefania; Kshirsagar, Giridhar U; 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; Kastrup, Jette Sandholm; Pickering, Darryl S.
Afiliação
  • Brogi S; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Brindisi M; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Butini S; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Kshirsagar GU; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Maramai S; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Chemi G; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Gemma S; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Campiani G; Department of Biotechnology, Chemistry and Pharmacy, (DoE 2018-2022) NatSynDrugs , University of Siena , Via A. Moro 2 , 53100 Siena , Italy.
  • Novellino E; Department of Pharmacy , University of Napoli Federico II , Via D. Montesano 49 , 80131 Napoli , Italy.
  • Fiorenzani P; Department of Medicine, Surgery and Neuroscience , University of Siena , Viale M. Bracci 16 , 53100 Siena , Italy.
  • Pinassi J; Department of Medicine, Surgery and Neuroscience , University of Siena , Viale M. Bracci 16 , 53100 Siena , Italy.
  • Aloisi AM; Department of Medicine, Surgery and Neuroscience , University of Siena , Viale M. Bracci 16 , 53100 Siena , Italy.
  • Gynther M; School of Pharmacy, Faculty of Health Sciences , University of Eastern Finland , 70211 Kuopio , Finland.
  • Venskutonyte R; Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.
  • Han L; Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.
  • Frydenvang K; Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.
  • Kastrup JS; Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.
  • Pickering DS; Department of Drug Design and Pharmacology , University of Copenhagen , Jagtvej 162 , DK-2100 Copenhagen , Denmark.
J Med Chem ; 61(5): 2124-2130, 2018 03 08.
Article em En | MEDLINE | ID: mdl-29451794
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 by 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).
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Ácido Caínico / Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiônico Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Itália
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Ácido Caínico / Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiônico Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Itália