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Synthesis and anti-tuberculosis activity of glycitylamines.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2016 Feb 15; Vol. 24 (4), pp. 693-702. Date of Electronic Publication: 2015 Dec 23. - Publication Year :
- 2016
-
Abstract
- A series of glycitylamines, which were prepared in few steps from readily available carbohydrates, were tested for their ability to inhibit tuberculosis growth in an Alamar Blue BCG colourimetric assay. Several derivatives, including (2R,3R)-1-(hexadecylamine)pent-4-ene-2,3-diol, (2R,3R)-1-(hexadecylmethylamino)pent-4-ene-2,3-diol and 5-deoxy-5-hexadecylmethylamino-D-arabinitol, were prepared in good to excellent (44-90%) overall yield and exhibited micromolar (20-41μM) inhibitory activity that was similar to the first line tuberculosis (TB) drug ethambutol (39μM) in the same assay. The ease and low cost of the synthesis of the glycitylamines offers definite advantages for their use as potential TB drugs.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amines chemical synthesis
Amines chemistry
Antitubercular Agents chemical synthesis
Antitubercular Agents chemistry
Colorimetry
Dose-Response Relationship, Drug
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship
Amines pharmacology
Antitubercular Agents pharmacology
Mycobacterium tuberculosis drug effects
Tuberculosis drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 24
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26810833
- Full Text :
- https://doi.org/10.1016/j.bmc.2015.12.036