SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 632-638, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-245035
ABSTRACT
Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Sulfathiazoles
/
Chemistry
/
Protein Tyrosine Phosphatase, Non-Receptor Type 1
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2014
Type:
Article
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