期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 2, 页码 532-537出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.084
关键词
sialidase; inhibitor design; DANA; selectivity; homology models; docking
We here report the design and synthesis of selective human lysosomal sialidase (NEU1) inhibitors. A series of amide-linked C9 modified DANA (2-deoxy-2,3-dehydro-N-acetylneuraminic acid) analogues were synthesized and their inhibitory activities against all four human sialidases (NEU1-NEU4) were determined. Structure-based approach was used to investigate the basis of selectivity of the compounds with experimentally observed activity. Results from the present study are found to be informative in a qualitative manner for the further design of isoform selective human sialidase inhibitors for therapeutic value. (c) 2007 Elsevier Ltd. All rights reserved.
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