A novel dipeptidyl peptidase IV inhibitors developed through scaffold hopping and drug splicing strategy
Wang, S.-C.; Zeng, L.-L.; Ding, Y.-Y.; Zeng, S.-G.; Song, H.-R.; Hu, W.-H.; Xie, H.
Yao Xue Xue Bao 49(1): 61-67
2014
ISSN/ISBN: 0513-4870 PMID: 24783507 Document Number: 675767
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.