期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 9, 页码 2619-2623出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.101
关键词
Chiral gossypol; Analog; Amino acid derivative; D-Glucosamine derivative; Avian influenza virus; Blocking viral entry
资金
- National Natural Science Foundation of China [30770228]
A series of chiral gossypol derivatives and its analogs were synthesized and tested in vitro for their anti-H5N1 activity. Interestingly, (+)-gossypol derivatives and its analogs were more active against H5N1 than the corresponding (-)-gossypol derivatives and its analogs. Through a simple chemical modification with amino acids, less active chiral gossypol could be converted into more active derivatives, and most of chiral gossypol derivatives were more potent against H5N1 than 1-adamantylamine. With regard to the mechanism of action, chiral gossypol derivatives and its analogs might impair the virus entry step of cell infection, likely targeting to HA2 protein. (C) 2013 Elsevier Ltd. All rights reserved.
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