Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 367-373, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-323034
ABSTRACT
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Drug Design
/
Molecular Structure
/
Chemistry
/
Inhibitory Concentration 50
/
Enzyme Inhibitors
/
Protein Tyrosine Phosphatase, Non-Receptor Type 1
/
Malonates
/
Metabolism
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
Similar
MEDLINE
...
LILACS
LIS