Pascal and Francis Bibliographic Databases

Help

Export

Selection :

Permanent link
http://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18811513

Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin

Author
BIFTU, Tesfaye1 ; SCAPIN, Giovanna1 ; SINHA-ROY, Ranabir3 ; BEI ZHANG3 ; WU, Joseph3 ; XIAOPING ZHANG3 ; DOSS, George A4 ; THORNBERRY, Nancy A3 ; WEBER, Ann E1 ; SINGH, Suresh1 ; FENG, Dennis1 ; BECKER, Joe W1 ; EIERMANN, George2 ; HUAIBING HE1 ; LYONS, Kathy1 ; PATEL, Sangita1 ; PETROV, Aleksandr2
[1] Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States
[2] Department of Pharmacology, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States
[3] Department of Metabolic Disorders, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States
[4] Department of Drug Metabolism, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, United States
Source

Bioorganic & medicinal chemistry letters (Print). 2007, Vol 17, Num 12, pp 3384-3387, 4 p

ISSN
0960-894X
Scientific domain
Biochemistry, molecular biology, biophysics; Pharmacology drugs
Publisher
Elsevier, Oxford
Publication country
United Kingdom
Document type
Article
Language
English
Author keyword
Cyclohexylamine DPP-4 Januvia Sitagliptin
Keyword (fr)
Activité biologique Analyse structurale Animal Biodisponibilité Chien Diabète Diffraction RX Dipeptidyl-peptidase IV In vivo Inhibiteur enzyme Modèle moléculaire Modélisation Pharmacocinétique Rat Singe Structure cristalline Synthèse chimique Voie orale 1,2,4-Triazolo[4,3-a]pyrazine dérivé 1,2,4-Triazolo[4,3-a]pyrazine(7-[3-amino-4-arylcyclohexyl]-5,6,7,8-tétrahydro-3-trifluorométhyl) Cyclohexylamine dérivé Inhibiteur DPIV Sitagliptine Triazolopyrazine Carnivora Endocrinopathie Enzyme Fissipedia Hydrolases Mammalia Peptidases Primates Rodentia Vertebrata
Keyword (en)
Biological activity Structural analysis Animal Bioavailability Dog Diabetes mellitus X ray diffraction Dipeptidyl-peptidase IV In vivo Enzyme inhibitor Molecular model Modeling Pharmacokinetics Rat Monkey Crystalline structure Chemical synthesis Oral administration Sitagliptin Carnivora Endocrinopathy Enzyme Fissipedia Hydrolases Mammalia Peptidases Primates Rodentia Vertebrata
Keyword (es)
Actividad biológica Análisis estructural Animal Biodisponibilidad Perro Diabetes Difracción RX Dipeptidyl-peptidase IV In vivo Inhibidor enzima Modelo molecular Modelización Farmacocinética Rata Mono Estructura cristalina Síntesis química Vía oral Sitagliptina Carnivora Endocrinopatía Enzima Fissipedia Hydrolases Mammalia Peptidases Primates 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
18811513

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

Searching the Web