Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B
- Author
- ANDERSEN, Henrik Sune; OLSEN, Ole H; MORAN, Edmond J; JING SU; BAKIR, Farid; JUDGE, Luke; SHAHBAZ, Manou; COLLINS, Tassie; VO, Todd; NEWMAN, Michael J; RIPKA, William C; MØLLER, Niels Peter H; IVERSEN, Lars F; SØRENSEN, Anette L. P; MORTENSEN, Steen B; CHRISTENSEN, Michael S; BRANNER, Sven; HANSEN, Thomas K; LAU, Jesper F; JEPPESEN, Lone
- Source
Journal of medicinal chemistry (Print). 2002, Vol 45, Num 20, pp 4443-4459, 17 p ; ref : 35 ref
- CODEN
- JMCMAR
- ISSN
- 0022-2623
- Scientific domain
- Pharmacology drugs
- Publisher
- American Chemical Society, Washington, DC
- Publication country
- United States
- Document type
- Article
- Language
- English
- Keyword (fr)
- Biodisponibilité Carboxamide Complexe enzyme inhibiteur Composé bicyclique Composé non peptide Cycle 5 chaînons Diffraction RX Hétérocycle soufre azote Hétérocycle soufre In vitro In vivo Inhibiteur enzyme Inhibition compétitive Isozyme Modèle moléculaire Modélisation Pharmacocinétique Protein-tyrosine-phosphatase Rat Relation structure activité Site actif Synthèse chimique Sélectivité Voie orale Benzo[b]thiophène-3-carboxylique acide dérivé Benzothiophène Oxamique acide(N-[2-carboxy-5-phényl-3-thiényl]) Oxamique acide(N-[3-carboxy-6-hydroxy-4,5,6,7-tétrahydrobenzo[b]thién-2-yl]) Oxamique acide(N-[3-carboxy-6-oxo-4,5,6,7-tétrahydrobenzo[b]thién-2-yl]) Oxamique acide(N-[3-carboxy-6-phénéthyl-4,5,6,7-tétrahydrothiéno[2,3-c]pyrid-2-yl]) Protein-tyrosine-phosphatase 1B Thiophène-2-carboxylique acide dérivé Thiéno[2,3-c]pyridine-3-carboxylique acide dérivé Thiénopyridine Enzyme Esterases Hydrolases Mammalia Phosphoric monoester hydrolases Rodentia Vertebrata
- Keyword (en)
- Bioavailability Carboxamide Inhibitor enzyme complex Bicyclic compound Non peptide compound Five membered ring X ray diffraction Sulfur nitrogen heterocycle Sulfur heterocycle In vitro In vivo Enzyme inhibitor Competitive inhibition Isozyme Molecular model Modeling Pharmacokinetics Protein-tyrosine-phosphatase Rat Structure activity relation Active site Chemical synthesis Selectivity Oral administration Enzyme Esterases Hydrolases Mammalia Phosphoric monoester hydrolases Rodentia Vertebrata
- Keyword (es)
- Biodisponibilidad Carboxamida Complejo enzima inhibidor Compuesto bicíclico Compuesto no péptido Ciclo 5 eslabones Difracción RX Heterociclo azufre nitrógeno Heterociclo azufre In vitro In vivo Inhibidor enzima Inhibición competitiva Isozima Modelo molecular Modelización Farmacocinética Protein-tyrosine-phosphatase Rata Relación estructura actividad Lugar activo Síntesis química Selectividad Vía oral Enzima Esterases Hydrolases Mammalia Phosphoric monoester hydrolases Rodentia Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02O Hormones. Endocrine system
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 13936691
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
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DOI
10.1021/jm0209026 
https://dx.doi.org/10.1021/jm0209026
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