Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes II: Optimisation of the PK profile
Tools
Tools
Sutton, J, Clark, D, Dunsdon, J, Fenton, G, Fillmore, A, Harris, N, Higgs, C, Hurley, C, Krintel, S, MacKenzie, R, Duttaroy, Alokesh, Gangl, Eric, Maniara, Wieslawa, Sedrani, Richard, Namoto, Kenji, Ostermann, Nils, Sirockin, Finton, Trappe, Joerg, Hassiepen, Ulrich and Baeschlin, Daniel (2011) Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes II: Optimisation of the PK profile. Bioorganic and medicinal chemistry letters, 22 (3). pp. 1464-1468. ISSN 0960-894X
Abstract
Optimisation of compounds from a series of deazaxanthines is described. SAR from the deazahypoxanthine series described previously was used to design improved deazaxanthine-based DPP-4 inhibitors which not only exhibited excellent activity and selectivity but showed improved in vivo activity due to an improved PK profile. Optimization of compound 1 resulted in the identification of compound 9i, which displayed good ex vivo DPP-4 inhibition and a superior PK profile in rat, potentially suitable for once daily dosing in man.
| Item Type: | Article |
|---|---|
| Related URLs: | |
| Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Dipeptidyl peptidase IV inhibitor; diabetes |
| Related URLs: | |
| Date Deposited: | 13 Oct 2015 13:15 |
| Last Modified: | 13 Oct 2015 13:15 |
| URI: | https://oak.novartis.com/id/eprint/5549 |