Aminomethylpyridines as DPP-IV inhibitors.
In a novel series of DPP-IV inhibitors, a large increase of inhibitory activity was achieved by optimisation of aromatic substituents and conformational restriction.
Peters
Jens-Uwe
JU
Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland. jens-uwe.peters@roche.com
Weber
Silja
S
Kritter
Stéphane
S
Weiss
Peter
P
Wallier
Angelina
A
Zimmerli
Daniel
D
Boehringer
Markus
M
Steger
Matthias
M
Loeffler
Bernd-Michael
BM
D000588:Amines / Q000737:chemistry*; D002478:Cells, Cultured; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D006841:Hydrocarbons, Aromatic / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000588:Amines; D004791:Enzyme Inhibitors; D006841:Hydrocarbons, Aromatic; D011725:Pyridines; D018819:Dipeptidyl Peptidase 4