A novel dipeptidyl peptidase IV inhibitors developed through scaffold hopping and drug splicing strategy / 药学学报
Acta Pharmaceutica Sinica
;
(12): 61-67, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-297970
ABSTRACT
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Piperidines
/
Structure-Activity Relationship
/
Uracil
/
Drug Design
/
Molecular Structure
/
Chemistry
/
Dipeptidyl-Peptidase IV Inhibitors
/
Drug Discovery
/
Linagliptin
/
Hypoglycemic Agents
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2014
Type:
Article
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