ankit_wjpps_(IF-2.78).pdf
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Diabetes affects 12% of the total population in world. So it is very<br>important to treat this fatal disease. There are many marketed<br>preparation is available to treat diabetes but not a single medicine have<br>the ability to cure it. A thirst in research area is more and more<br>increased now a day. Novel pathways and targets are identified in<br>current time that may be kill this dragon named diabetes. Inhibition of<br>a novel target PTP1B is chosen for attack on diabetes. PTP1B<br>inhibition reported as negative regulator of insulin signaling pathway<br>which increased the insulin sensitivity on insulin receptor. The<br>numerous scaffold are reported and still so much research task going<br>on for PTP1B inhibition. We choose Hydantoin scaffold as novel<br>inhibition of PTP1B and design molecule that binds with this enzyme<br>and inhibit it. A series of substituted 2-[4-[(2,5-dioxo imidazolidin-4- ylidene) methyl]<br>Aryloxy] -N-arylacetamide is decided to synthesized. The inhibition of PTP1B is in vitro<br>tested over PTP1B enzymatic kit. Among all the tested compounds, two compound were<br>found most potent activity 90.59% & 97.56 % inhibition respecively (N-(4-bromophenyl)-2-<br>[4-[(2,5- dioxoimidazolidin-4-ylidene)methyl] phenoxy]acetamides) and (2-[[2-[4-[(2,5-dioxoimidazolidin-4-ylidene)methyl] phenoxy] acetyl]amino]benzoic acid) with compared to<br>standard drug suramin.
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figshare
创建时间:
2016-09-21



