Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 367-373, 2012.
Article
Dans Chinois
| 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.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Relation structure-activité
/
Conception de médicament
/
Structure moléculaire
/
Chimie
/
Concentration inhibitrice 50
/
Antienzymes
/
Protein Tyrosine Phosphatase, Non-Receptor Type 1
/
Malonates
/
Métabolisme
Limites du sujet:
Humains
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2012
Type:
Article
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