Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Arora, Inderpreet
Kashyap, V K Singh, A K Dasgupta, Arunava Kumar, Brijesh Shaw, A K |
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| Date |
2014-10-01T05:18:55Z
2014-10-01T05:18:55Z 2014 |
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| Identifier |
Organic & Biomolecular Chemistry, 2014, 12(35):6855-68
http://hdl.handle.net/123456789/1417 |
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| Description |
Principle guided design of glycan processing enzyme inhibitors involves embedding aromatic group onto charge and shape mimics. Intramolecular azide-alkyne cycloaddition was used as a simple and versatile strategy for the synthesis of novel condensed bicyclic triazoles from carbohydrate derived Perlin aldehydes. These newly synthesised molecules were evaluated for glycosidase inhibition against 11 commercially available enzymes and were found to posess significant affinity (micromolar range) as well as high degree of selectivity for α-glucosidases. Conformational restriction was identified as an important tool to customize the selectivity of enzyme inhibition by five-membered iminosugar
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593919 bytes
application/pdf |
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| Language |
en
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| Relation |
CSIR-CDRI Communication No. 8730
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| Subject |
Synthesis and Biological evaluation
Bicyclic Iminosugar Hybrids Conformational constraint Selectivity of α-glucosidase |
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| Title |
Design, Synthesis and Biological evaluation of Bicyclic Iminosugar Hybrids: Conformational constraint as an effective tool for tailoring the selectivity of α-glucosidase inhibitors
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| Type |
Article
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