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Synthesis, modification and biological activity of 2,3-indoles of Glycyrrhetinic acid. | LitMetric

The synthesis of 2,3-indoles of Glycyrrhetinic acid (GLA) and its methyl ester was carried out by the Fischer reaction. Reductive transformations of GLA methyl ester 2,3-indole were carried out to obtain 11-deoxo- and 9,12-diene analogs. N-methylation of 2,3-indole gave N-methyl-indole-11-oxo-18β-olean-12-en-30-oic acid. The antiulcer and anti-inflammatory activity of 2,3-indole was studied in rats and mice. It was found, compound exhibied a pronounced antiulcer activity in the indomethacin model of ulcers in rats and anti-inflammatory activity in the carrageenan model of acute edoema in mice, at a dose of 50 mg/kg. This is the first report of anti-ulcer and anti-inflammatory activities of 2,3-indolo-GLA derivatives.

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http://dx.doi.org/10.1080/14786419.2024.2326844DOI Listing

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