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Synthesis, Structure Elucidation and H+/K+-ATPase Inhibitory Activity of Bisabolangelone Reduction Derivatives
- Source :
- Chinese Journal of Chemistry. 30:71-76
- Publication Year :
- 2011
- Publisher :
- Wiley, 2011.
-
Abstract
- Nine bisabolangelone reduction derivatives were synthesized and separated as potential anti-ulcer agent. Their structures were characterized by 2D NMR, IR, ESI-MS, elemental analysis and single-crystal X-ray diffraction analysis. Preliminarily H+/K+-ATPase activity evaluation indicated that all the target compounds had a certain inhibitory effect, and compounds II and IV exhibited the better inhibitory activity against H+/K+-ATPase than bisabolangelone and the commercial omeprazole with the IC50 of 23.21 and 65.32 μmol/L, respectively. The initial structure-activity analysis suggested that the presence of carbonyl group in six-membered ring and double bond in side-chain seemed to be necessary to the activity.
- Subjects :
- chemistry.chemical_classification
biology
Double bond
Chemistry
Stereochemistry
ATPase
General Chemistry
Inhibitory postsynaptic potential
Medicinal chemistry
Carbonyl group
Bisabolangelone
chemistry.chemical_compound
X-ray crystallography
biology.protein
IC50
Two-dimensional nuclear magnetic resonance spectroscopy
Subjects
Details
- ISSN :
- 1001604X
- Volume :
- 30
- Database :
- OpenAIRE
- Journal :
- Chinese Journal of Chemistry
- Accession number :
- edsair.doi...........b2b28b9c497402ffc3eb0297a740b0e8