Studies on n-octyl-5-(alpha-D-arabinofuranosyl)-beta-D-galactofuranosides for mycobacterial glycosyltransferase activity
| Autor: | Ashish K. Pathak, Robert C. Reynolds, Vibha Pathak, Sudagar S Gurcha, Joseph A. Maddry, Gurdyal S. Besra, Caroline B. Morehouse, William J. Suling |
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| Rok vydání: | 2002 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Molecular Sequence Data Disaccharide Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Disaccharides Biochemistry Mycobacterium Substrate Specificity chemistry.chemical_compound Biosynthesis Drug Discovery Glycosyltransferase Pentosyltransferases Enzyme Inhibitors Glycosyl donor Molecular Biology Antibacterial agent chemistry.chemical_classification biology Organic Chemistry Polysaccharides Bacterial Glycosyltransferases Mycobacterium tuberculosis In vitro Enzyme chemistry Carbohydrate Sequence Enzyme inhibitor biology.protein Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry. 10(4) |
| ISSN: | 0968-0896 |
| Popis: | The mycobacterial cell wall is a potential target for new drug development. Herein we report the preparation and activity of several n -octyl-5-(α- d -arabinofuranosyl)-β- d -galactofuranoside derivatives. A cell-free assay system has been utilized for determination of the ability of disaccharide analogues to act as arabinosyltransferase acceptors using [ 14 C]-DPA as the glycosyl donor. In addition, in vitro inhibitory activity has been determined in a colorimetric broth microdilution assay system against MTB H37Ra and three clinical isolates of Mycobacterium avium complex (MAC). One of these disaccharides showed moderate activity against MTB. The biological evaluation of these disaccharides suggests that more hydrophobic analogues with a blocked reducing end showed better activity as compared to a totally deprotected disaccharide that more closely resembles the natural substrates in cell wall biosynthesis. |
| Databáze: | OpenAIRE |
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