Synthesis and biological activities of novel indole derivatives as potent and selective PPARγ modulators
- Author
- LAMOTTE, Yann1 ; MARTRES, Paul1 ; FAUCHER, Nicolas1 ; LAROZE, Alain1 ; GRILLOT, Didier2 ; ANCELLIN, Nicolas2 ; SAINTILLAN, Yannick2 ; BENETON, Véronique3 ; GAMPE, Robert T4
[1] Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France
[2] Department of Biology, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France
[3] Department of Drugs Metabolism and Pharmacokinetics, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France
[4] Department of Computational and Structural Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, United States - Source
Bioorganic & medicinal chemistry letters (Print). 2010, Vol 20, Num 4, pp 1399-1404, 6 p
- ISSN
- 0960-894X
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- Diabetes Modulator PPARy Peroxisome proliferator-activated receptor Telmisartan
- Keyword (fr)
- Activité biologique Animal Diabète Dérivé de l'indole Dérivé du biphényle Glucose Homme In vitro In vivo Mode liaison Rat Récepteur PPAR-γ Récepteur nucléaire Souris Synthèse chimique Sélectivité Telmisartan Triglycéride Voie orale Biphényle-2-carboxylique acide(4p-[2,3-diméthyl-5-(1-phénylpropylcarbamaoyl)indol-1-ylméthyl]) Indole-5-carboxamide dérivé Modulateur sélectif récepteur PPAR Endocrinopathie Mammalia Rodentia Vertebrata
- Keyword (en)
- Biological activity Animal Diabetes mellitus Indole derivatives Biphenyl derivatives Glucose Human In vitro In vivo Binding mode Rat PPAR-γ receptor Nuclear receptor Mouse Chemical synthesis Selectivity Telmisartan Triglyceride Oral administration Selective PPAR modulator Endocrinopathy Mammalia Rodentia Vertebrata
- Keyword (es)
- Actividad biológica Animal Diabetes Indol derivado Bifenilo derivado Glucosa Hombre In vitro In vivo Modo de enlace Rata Receptor PPAR-γ Receptor nuclear Ratón Síntesis química Selectividad Telmisartán Triglicérido Vía oral Endocrinopatía Mammalia Rodentia Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02N General and cellular metabolism. Vitamins
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 22824709
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
Access to the document
Install on your browser
DOI
10.1016/j.bmcl.2009.12.107 
https://dx.doi.org/10.1016/j.bmcl.2009.12.107
"O:13:\"PanistOpenUrl\":36:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000idc\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2009.12.107\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2010\";s:9:\"\u0000*\u0000volume\";s:2:\"20\";s:8:\"\u0000*\u0000issue\";s:1:\"4\";s:8:\"\u0000*\u0000spage\";s:4:\"1399\";s:8:\"\u0000*\u0000epage\";s:4:\"1404\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:7:\"LAMOTTE\";s:10:\"\u0000*\u0000aufirst\";s:4:\"Yann\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:8:{i:0;s:13:\"MARTRES, Paul\";i:1;s:16:\"FAUCHER, Nicolas\";i:2;s:13:\"LAROZE, Alain\";i:3;s:15:\"GRILLOT, Didier\";i:4;s:17:\"ANCELLIN, Nicolas\";i:5;s:19:\"SAINTILLAN, Yannick\";i:6;s:19:\"BENETON, V\u00e9ronique\";i:7;s:15:\"GAMPE, Robert T\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"6\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Panist access
"O:12:\"IstexOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2009.12.107\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2010\";s:9:\"\u0000*\u0000volume\";s:2:\"20\";s:8:\"\u0000*\u0000issue\";s:1:\"4\";s:8:\"\u0000*\u0000spage\";s:4:\"1399\";s:8:\"\u0000*\u0000epage\";s:4:\"1404\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:7:\"LAMOTTE\";s:10:\"\u0000*\u0000aufirst\";s:4:\"Yann\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:8:{i:0;s:13:\"MARTRES, Paul\";i:1;s:16:\"FAUCHER, Nicolas\";i:2;s:13:\"LAROZE, Alain\";i:3;s:15:\"GRILLOT, Didier\";i:4;s:17:\"ANCELLIN, Nicolas\";i:5;s:19:\"SAINTILLAN, Yannick\";i:6;s:19:\"BENETON, V\u00e9ronique\";i:7;s:15:\"GAMPE, Robert T\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"6\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Istex access
"O:16:\"UnpaywallOpenUrl\":35:{s:8:\"\u0000*\u0000email\";s:27:\"assistance-portail@inist.fr\";s:6:\"\u0000*\u0000fmt\";N;s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2009.12.107\";s:6:\"\u0000*\u0000pii\";N;s:7:\"\u0000*\u0000pmid\";N;s:9:\"\u0000*\u0000atitle\";N;s:9:\"\u0000*\u0000jtitle\";N;s:9:\"\u0000*\u0000stitle\";N;s:7:\"\u0000*\u0000date\";N;s:9:\"\u0000*\u0000volume\";N;s:8:\"\u0000*\u0000issue\";N;s:8:\"\u0000*\u0000spage\";N;s:8:\"\u0000*\u0000epage\";N;s:8:\"\u0000*\u0000pages\";N;s:7:\"\u0000*\u0000issn\";N;s:8:\"\u0000*\u0000eissn\";N;s:9:\"\u0000*\u0000aulast\";N;s:10:\"\u0000*\u0000aufirst\";N;s:9:\"\u0000*\u0000auinit\";N;s:10:\"\u0000*\u0000auinitm\";N;s:5:\"\u0000*\u0000au\";N;s:9:\"\u0000*\u0000aucorp\";N;s:7:\"\u0000*\u0000isbn\";N;s:8:\"\u0000*\u0000coden\";N;s:8:\"\u0000*\u0000genre\";N;s:7:\"\u0000*\u0000part\";N;s:9:\"\u0000*\u0000btitle\";N;s:8:\"\u0000*\u0000title\";N;s:8:\"\u0000*\u0000place\";N;s:6:\"\u0000*\u0000pub\";N;s:10:\"\u0000*\u0000edition\";N;s:9:\"\u0000*\u0000tpages\";N;s:9:\"\u0000*\u0000series\";N;s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";N;}"
Unpaywall access
"O:16:\"EuropePMCOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2009.12.107\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2010\";s:9:\"\u0000*\u0000volume\";s:2:\"20\";s:8:\"\u0000*\u0000issue\";s:1:\"4\";s:8:\"\u0000*\u0000spage\";s:4:\"1399\";s:8:\"\u0000*\u0000epage\";s:4:\"1404\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:7:\"LAMOTTE\";s:10:\"\u0000*\u0000aufirst\";s:4:\"Yann\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:8:{i:0;s:13:\"MARTRES, Paul\";i:1;s:16:\"FAUCHER, Nicolas\";i:2;s:13:\"LAROZE, Alain\";i:3;s:15:\"GRILLOT, Didier\";i:4;s:17:\"ANCELLIN, Nicolas\";i:5;s:19:\"SAINTILLAN, Yannick\";i:6;s:19:\"BENETON, V\u00e9ronique\";i:7;s:15:\"GAMPE, Robert T\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"6\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
Europe PubMed Central access
"O:12:\"ArXivOpenUrl\":35:{s:10:\"\u0000*\u0000openUrl\";N;s:6:\"\u0000*\u0000fmt\";s:7:\"journal\";s:6:\"\u0000*\u0000doi\";s:26:\"10.1016\/j.bmcl.2009.12.107\";s:6:\"\u0000*\u0000pii\";s:0:\"\";s:7:\"\u0000*\u0000pmid\";s:0:\"\";s:9:\"\u0000*\u0000atitle\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:9:\"\u0000*\u0000jtitle\";s:48:\"Bioorganic & medicinal chemistry letters (Print)\";s:9:\"\u0000*\u0000stitle\";s:32:\"Bioorg. med. chem. lett. (Print)\";s:7:\"\u0000*\u0000date\";s:4:\"2010\";s:9:\"\u0000*\u0000volume\";s:2:\"20\";s:8:\"\u0000*\u0000issue\";s:1:\"4\";s:8:\"\u0000*\u0000spage\";s:4:\"1399\";s:8:\"\u0000*\u0000epage\";s:4:\"1404\";s:8:\"\u0000*\u0000pages\";s:0:\"\";s:7:\"\u0000*\u0000issn\";s:9:\"0960-894X\";s:8:\"\u0000*\u0000eissn\";s:0:\"\";s:9:\"\u0000*\u0000aulast\";s:7:\"LAMOTTE\";s:10:\"\u0000*\u0000aufirst\";s:4:\"Yann\";s:9:\"\u0000*\u0000auinit\";s:0:\"\";s:10:\"\u0000*\u0000auinitm\";s:0:\"\";s:5:\"\u0000*\u0000au\";a:8:{i:0;s:13:\"MARTRES, Paul\";i:1;s:16:\"FAUCHER, Nicolas\";i:2;s:13:\"LAROZE, Alain\";i:3;s:15:\"GRILLOT, Didier\";i:4;s:17:\"ANCELLIN, Nicolas\";i:5;s:19:\"SAINTILLAN, Yannick\";i:6;s:19:\"BENETON, V\u00e9ronique\";i:7;s:15:\"GAMPE, Robert T\";}s:9:\"\u0000*\u0000aucorp\";s:0:\"\";s:7:\"\u0000*\u0000isbn\";s:0:\"\";s:8:\"\u0000*\u0000coden\";s:0:\"\";s:8:\"\u0000*\u0000genre\";s:7:\"article\";s:7:\"\u0000*\u0000part\";s:0:\"\";s:9:\"\u0000*\u0000btitle\";s:0:\"\";s:8:\"\u0000*\u0000title\";s:105:\"Synthesis and biological activities of novel indole derivatives as potent and selective PPAR\u03b3 modulators\";s:8:\"\u0000*\u0000place\";s:9:\"Amsterdam\";s:6:\"\u0000*\u0000pub\";s:8:\"Elsevier\";s:10:\"\u0000*\u0000edition\";s:0:\"\";s:9:\"\u0000*\u0000tpages\";s:1:\"6\";s:9:\"\u0000*\u0000series\";s:0:\"\";s:8:\"\u0000*\u0000proxy\";s:30:\"http:\/\/proxyout.inist.fr:8080\/\";s:12:\"\u0000*\u0000integrite\";b:1;}"
arXiv access
