Kayet, Anirban ; Datta, Dhrubajyoti ; Das, Ashrukana ; Dasgupta, Swagata ; Pathak, Tanmaya (2018) 1,5-disubstituted 1,2,3-triazole linked disaccharides: metal-free syntheses and screening of a new class of ribonuclease A inhibitors Bioorganic & Medicinal Chemistry, 26 (2). pp. 455-462. ISSN 0968-0896
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Official URL: https://www.sciencedirect.com/science/article/pii/...
Related URL: http://dx.doi.org/10.1016/j.bmc.2017.12.004
Abstract
1,5-Regioisomeric triazole linked disaccharides have been synthesized and screened for their inhibitory properties against ribonuclease A (RNase A). The angular constraint-driven 'crescent shaped' inhibitors accommodated themselves into the enzyme active site. An improved enzyme inhibition was observed with increased H-bonding ability of polar functional groups in the modified disaccharides. In this series, introduction of two carboxyl groups in the furanose rings elicited the best result with an inhibition constant of 50 ± 3 µM. This is the first ever report on the use of disaccharides as RNase A inhibitors.
Item Type: | Article |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | Disaccharides; Vinyl Sulfone; 1,5-Disubstituted-triazole; Inhibitors; Ribonuclease A |
ID Code: | 113312 |
Deposited On: | 10 May 2018 11:45 |
Last Modified: | 10 May 2018 11:45 |
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