Singh, Fateh V. ; Parihar, Amrita ; Chaurasia, Sumit ; Singh, Amar B. ; Singh, Salil P. ; Tamrakar, Akhilesh K. ; Srivastava, Arvind K. ; Goel, Atul (2009) 5,6-Diarylanthranilo-1,3-dinitriles as a new class of antihyperglycemic agents Bioorganic & Medicinal Chemistry Letters, 19 (8). pp. 2158-2161. ISSN 0960-894X
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Official URL: http://doi.org/10.1016/j.bmcl.2009.02.118
Related URL: http://dx.doi.org/10.1016/j.bmcl.2009.02.118
Abstract
Various functionalized mono- and diarylanthranilo-1,3-dinitriles were synthesized and evaluated for their in vitro antihyperglycemic activity against the PTP-1B, glucose-6-phosphatase, glycogen phosphorylase and α-glucosidase enzymes. Among various screened compounds, 5,6-diaryl substituted anthranilo-1,3-dinitriles 3a, 3b, and 3d showed good inhibitory activity against PTP-1B with IC50 values of 58–72 μM. Three of the test compounds showed significant (25–37%) lowering of plasma glucose level at 24 h in sucrose-challenged streptozotocin-induced diabetic Sprague–Dawley rat model.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Diarylanthranilo-1,3-dinitriles1,2-Teraryl; PTP 1B Inhibitor; STZ-S Model; Antihyperglycemic. |
| ID Code: | 117938 |
| Deposited On: | 06 May 2021 09:53 |
| Last Modified: | 06 May 2021 09:53 |
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