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https://hdl.handle.net/2440/34861
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Type: | Journal article |
Title: | Ring-deactivated hydroxyalkylpyrrole-based inhibitors of alpha-chymotrypsin: synthesis and mechanism of action |
Author: | Martyn, D. Vernall, A. Clark, B. Abell, A. |
Citation: | Organic and Biomolecular Chemistry, 2003; 1(12):2103-2110 |
Publisher: | Royal Soc Chemistry |
Issue Date: | 2003 |
ISSN: | 1477-0520 1477-0539 |
Abstract: | 13C NMR and mass spectrometry studies have been used to demonstrate that the inhibition of alpha-chymotrypsin by N-sulfonylhydroxymethylpyrrole inhibitors (10) is non-covalent. Hydroxyalkylpyrroles in which an electron-withdrawing group (acyl substituent) is introduced at the alternative C2 position have been synthesised and also shown to inactivate alpha-chymotrypsin. SAR studies on this class suggests that the incorporation of phenylalanine at C2 is favoured, however, there is little gain in introducing a hydrophobic substituent at C5. |
Keywords: | Animals Cattle Pyrroles Chymotrypsin Serine Proteinase Inhibitors Structure-Activity Relationship |
DOI: | 10.1039/b302411c |
Description (link): | http://www.ncbi.nlm.nih.gov/pubmed/12945901 |
Published version: | http://dx.doi.org/10.1039/b302411c |
Appears in Collections: | Aurora harvest Chemistry publications |
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