Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs |
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Authors: | Chao Wang Tian-Tai Zhang Guan-Hua Du |
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Affiliation: | State Key Laboratory of Bioactive Substances and Functions of Natural Medicines , Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College , Beijing, 100050, China |
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Abstract: | The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed. |
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Keywords: | gaultherin analogs phase-transfer catalytic method anti-nociceptive anti-inflammatory |
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