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5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties
[Image: see text] Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure–activity relationship studies are pres...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2016
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4948010/ https://www.ncbi.nlm.nih.gov/pubmed/27437074 http://dx.doi.org/10.1021/acsmedchemlett.6b00145 |
| _version_ | 1782443267207462912 |
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| author | Kohn, Todd J. Du, Xiaohui Lai, SuJen Xiong, YuMei Komorowski, Renee Veniant, Murielle Fu, Zice Jiao, Xianyun Pattaropong, Vatee Chow, David Cardozo, Mario Jin, Lixia Conn, Marion DeWolf, Walter E. Kraser, Christopher F. Hinklin, Ronald J. Boys, Mark L. Medina, Julio C. Houze, Jonathan Dransfield, Paul Coward, Peter |
| author_facet | Kohn, Todd J. Du, Xiaohui Lai, SuJen Xiong, YuMei Komorowski, Renee Veniant, Murielle Fu, Zice Jiao, Xianyun Pattaropong, Vatee Chow, David Cardozo, Mario Jin, Lixia Conn, Marion DeWolf, Walter E. Kraser, Christopher F. Hinklin, Ronald J. Boys, Mark L. Medina, Julio C. Houze, Jonathan Dransfield, Paul Coward, Peter |
| author_sort | Kohn, Todd J. |
| collection | PubMed |
| description | [Image: see text] Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure–activity relationship studies are presented along with relevant pharmacokinetic and in vivo data. |
| format | Online Article Text |
| id | pubmed-4948010 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2016 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-49480102017-07-14 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties Kohn, Todd J. Du, Xiaohui Lai, SuJen Xiong, YuMei Komorowski, Renee Veniant, Murielle Fu, Zice Jiao, Xianyun Pattaropong, Vatee Chow, David Cardozo, Mario Jin, Lixia Conn, Marion DeWolf, Walter E. Kraser, Christopher F. Hinklin, Ronald J. Boys, Mark L. Medina, Julio C. Houze, Jonathan Dransfield, Paul Coward, Peter ACS Med Chem Lett [Image: see text] Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure–activity relationship studies are presented along with relevant pharmacokinetic and in vivo data. American Chemical Society 2016-06-01 /pmc/articles/PMC4948010/ /pubmed/27437074 http://dx.doi.org/10.1021/acsmedchemlett.6b00145 Text en Copyright © 2016 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
| spellingShingle | Kohn, Todd J. Du, Xiaohui Lai, SuJen Xiong, YuMei Komorowski, Renee Veniant, Murielle Fu, Zice Jiao, Xianyun Pattaropong, Vatee Chow, David Cardozo, Mario Jin, Lixia Conn, Marion DeWolf, Walter E. Kraser, Christopher F. Hinklin, Ronald J. Boys, Mark L. Medina, Julio C. Houze, Jonathan Dransfield, Paul Coward, Peter 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties |
| title | 5-Alkyl-2-urea-Substituted Pyridines: Identification
of Efficacious Glucokinase Activators with Improved Properties |
| title_full | 5-Alkyl-2-urea-Substituted Pyridines: Identification
of Efficacious Glucokinase Activators with Improved Properties |
| title_fullStr | 5-Alkyl-2-urea-Substituted Pyridines: Identification
of Efficacious Glucokinase Activators with Improved Properties |
| title_full_unstemmed | 5-Alkyl-2-urea-Substituted Pyridines: Identification
of Efficacious Glucokinase Activators with Improved Properties |
| title_short | 5-Alkyl-2-urea-Substituted Pyridines: Identification
of Efficacious Glucokinase Activators with Improved Properties |
| title_sort | 5-alkyl-2-urea-substituted pyridines: identification
of efficacious glucokinase activators with improved properties |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4948010/ https://www.ncbi.nlm.nih.gov/pubmed/27437074 http://dx.doi.org/10.1021/acsmedchemlett.6b00145 |
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