[A novel dipeptidyl peptidase IV inhibitors developed through scaffold hopping and drug splicing strategy].
Though all the marketed drugs of dipeptidyl peptidase IV inhibitors are structurally different, their inherent correlation is worthy of further investigation. Herein we rapidly discovered a novel DPP-IV inhibitor 8g (IC50 = 4.9 nmol.L-1) which exhibits as good activity and selectivity as the market drugs through scaffold hopping and drug splicing strategies based on alogliptin and linagliptin. This study demonstrated that the employment of classic medicinal chemistry strategy to the marketed drugs with specific target is an efficient approach to discover novel bioactive molecules.
Shan-Chun
SC
Wang
Li-Li
LL
Zeng
Yu-Yang
YY
Ding
Shao-Gao
SG
Zeng
Hong-Rui
HR
Song
Wen-Hui
WH
Hu
Hui
H
Xie
D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D000069476:Linagliptin / Q000138:chemical synthesis / Q000737:chemistry; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship; D014498:Uracil / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry
D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D010880:Piperidines; D000069476:Linagliptin; D014498:Uracil; C520853:alogliptin