Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: selective inhibitors of lysosomal sialidase (NEU1).
Article Details
- CitationCopy to clipboard
Magesh S, Moriya S, Suzuki T, Miyagi T, Ishida H, Kiso M
Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: selective inhibitors of lysosomal sialidase (NEU1).
Bioorg Med Chem Lett. 2008 Jan 15;18(2):532-7. Epub 2007 Nov 28.
- PubMed ID
- 18068975 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 2-deoxy-2,3-dehydro-N-acetylneuraminic acid Sialidase-2 IC 50 (nM) 43000 N/A N/A Details