Almtraet--The results of a structure-activity relationship study focusing on the interaction of a series of phthalimide and saccharin derivatives with leukocyte elastase, cathepsin G and proteinase 3 are described. The phthalimide derivatives were found to be inactive while some of the saccharin der
✦ LIBER ✦
Pitfalls in the synthesis and biological evaluation of sialyl-LewisX mimetics as potential selectin antagonists
✍ Scribed by Gerhard Kretzschmar; Alexander Toepfer; Christoph Hüls; Manfred Krause
- Publisher
- Elsevier Science
- Year
- 1997
- Tongue
- French
- Weight
- 539 KB
- Volume
- 53
- Category
- Article
- ISSN
- 0040-4020
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✦ Synopsis
The lower molecular weight analog 12 of sialyl Lewis x was prepared and effected equal binding affinity to E-and P-selectin compared to the parent tetrasaccharide. If 12 was prepared using acidic ion exchange resins, false positive test were produced, especially binding to P-selectin seemed to be considerably enhanced. Traces of polyanions released from the resins which are difficult to detect by routine analysis were identified to be highly potent selectin inhibitors, probably by their action on a non-carbohydrate binding site.
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