期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 26, 期 2, 页码 455-462出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.12.004
关键词
Disaccharides; Vinyl sulfone; 1,5-Disubstituted-triazole; Inhibitors; Ribonuclease A
资金
- Department of Biotechnology, Ministry of Science and Technology, New Delhi [BT/PR6189/BRB/10/1150/2012]
- Council of Scientific and Industrial Research, New Delhi
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 mu M. This is the first ever report on the use of disaccharides as RNase A inhibitors. (C) 2017 Elsevier Ltd. All rights reserved.
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