A potent dipeptide inhibitor of dipeptidyl peptidase IV.
A series of novel potent inhibitors of dipeptidyl peptidase IV (DPP-IV) has been developed. A brief structure-activity relationship of the inhibitors was investigated. The dipeptide TSL-225, tryptophyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, was identified with the critical structure for the inhibitory activity.
Yamada
M
M
Lead Generation Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Okagaki
C
C
Higashijima
T
T
Tanaka
S
S
Ohnuki
T
T
Sugita
T
T
D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects*; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines
D007546:Isoquinolines; D015842:Serine Proteinase Inhibitors; C115967:TSL 225; D044005:Tetrahydroisoquinolines; D018819:Dipeptidyl Peptidase 4