5, 6-Diarylanthranilo-1,3-dinitriles as a new class of antihyperglycemic agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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Creator |
Singh, F V
Parihar, Amrita Chaurasia, Sumit Singh, Amar B Singh, S P Tamrakar, A K Srivastava, A K Goel, Atul |
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Date |
2009-08-31T06:34:52Z
2009-08-31T06:34:52Z 2009 |
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Identifier |
Bioorg. Med. Chem. Lett.(2009) 19, 2158-2161
http://hdl.handle.net/123456789/485 |
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Description |
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 alpha-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 alphaM. Three of the test compounds showed significant (25-37%) lowering of plasma glucose level at 24 h in sucrose-challenged streptozotocin-induced diabetic Sprangue-Dawley rat model.
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Format |
165426 bytes
application/pdf |
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Language |
en
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Relation |
CDRI communication number 7335
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Title |
5, 6-Diarylanthranilo-1,3-dinitriles as a new class of antihyperglycemic agents
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Type |
Article
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