Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594787 | Bioorganic & Medicinal Chemistry Letters | 2014 | 32 Pages |
Abstract
The successful launches of dipeptidyl peptidase IV (DPP IV) inhibitors as oral anti-diabetics warrant and spur the further quest for additional chemical entities in this promising class of therapeutics. Numerous pharmaceutical companies have pursued their proprietary candidates towards the clinic, resulting in a large body of published chemical structures associated with DPP IV. Herein, we report the discovery of a novel chemotype for DPP IV inhibition based on the C-(1-aryl-cyclohexyl)-methylamine scaffold and its optimization to compounds which selectively inhibit DPP IV at low-nM potency and exhibit an excellent oral pharmacokinetic profile in the rat.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kenji Namoto, Finton Sirockin, Nils Ostermann, Francois Gessier, Stefanie Flohr, Richard Sedrani, Bernd Gerhartz, Jörg Trappe, Ulrich Hassiepen, Alokesh Duttaroy, Suzie Ferreira, Jon M. Sutton, David E. Clark, Garry Fenton, Mandy Beswick,