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Discovery of novel PTP1B inhibitors with antihyperglycemic activity

   
@article{APS7299,
	author = {Zhang Liu and Qian Chai and Yuan-yuan Li and Qiang Shen and Lan-ping Ma and Li-na Zhang and Xin Wang and Li Sheng and Jing-ya Li and Jia Li and Jing-kang Shen},
	title = {Discovery of novel PTP1B inhibitors with antihyperglycemic activity},
	journal = {Acta Pharmacologica Sinica},
	volume = {31},
	number = {8},
	year = {2016},
	keywords = {},
	abstract = {Aim: To discover and optimize a series of novel PTP1B inhibitors containing a thiazolidinone-substituted biphenyl scaffold and to further evaluate the inhibitory effects of these compounds in vitro and in vivo.
Methods: A total of 36 thiazolidinone substituted biphenyl scaffold derivatives were prepared. An in vitro biological evaluation was done by Enzyme-based assay. The in vivo efficacy of 7Fb as an antihyperglycemic agent was evaluated in a BKS db/db diabetic mouse model with a dose of 50 mg·kg-1·d-1 for 4 weeks.
Results: The in vitro biological evaluation showed that compounds 7Fb and 7Fc could increase the insulin-induced tyrosine phosphorylation of IRβ in CHO/hIR cells. In in vivo experiments, compound 7Fb significantly lowered the postprandial blood glucose, from 29.4±1.2 mmol/L with the vehicle to 24.7±0.6 mmol/L (P},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/7299}
}