Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structure-activity relationships

被引：10
|
作者：
Gupta, Swati [1 ]
Varshney, Kanika [1 ]
Srivastava, Rohit [2 ]
Rahuja, Neha [2 ]
Rawat, Arun K. [2 ]
Srivastava, Arvind K. [2 ]
Saxena, Anil K. [1 ]
机构：
[1] Cent Drug Res Inst, CSIR, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, CSIR, Div Biochem, Lucknow 226001, Uttar Pradesh, India
来源：
MEDCHEMCOMM | 2013年 / 4卷 / 10期
关键词：
TYROSINE-PHOSPHATASE; 1B; INSULIN SENSITIVITY; RESISTANCE; OBESITY; DISCOVERY; DESIGN;
D O I：
10.1039/c3md00138e
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The protein tyrosine phosphatase 1B (PTP1B) is an attractive target for the treatment of type 2 diabetes. A series of substituted 1,3-benzyl urea has been synthesized and evaluated for PTP1B inhibitory, antidiabetic and antidyslipidemic activities. The most active compound of the series 5b showed 79.4% PTP1B inhibition and 20.7% blood glucose lowering in the STZ model. It also lowered the serum cholesterol level by 16.3% and significantly increased the serum HDL-cholesterol by 46.8%. The high activity of compound 5b has been explained by docking studies.
引用
收藏
页码：1382 / 1387
页数：6
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