期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 24, 页码 6549-6554出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.10.071
关键词
Dengue virus NS2B-NS3 protease; Methionine-proline anilides; Proline; Methionine; 4-Nitroaniline
资金
- Natural Science Foundation of China [U0632001]
A series of methionine-proline dipeptide derivatives and their analogues were designed, synthesized and assayed against the serotype 2 dengue virus NS2B-NS3 protease, and methionine-proline anilides 1 and 2 were found to be the most active DENV 2 NS2B-NS3 competitive inhibitors with K-i values of 4.9 and 10.5 mu M. The structure and activity relationship and the molecular docking revealed that L-proline, L-methionine and p-nitroaniline in 1 and 2 are the important characters in blocking the active site of NS2B-NS3 protease. Our current results suggest that the title dipeptidic scaffold represents a promising structural core to discover a new class of active NS2B-NS3 competitive inhibitors. (C) 2013 Elsevier Ltd. All rights reserved.
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