Rutaecarpin analogue as well as preparation method and application thereof

The invention relates to a rutaecarpin analogue as well as a preparation method and application thereof, and belongs to the field of pharmaceutical chemistry synthesis. A 4 (3H)-quinazolinone derivative is used as a substrate, iron phthalocyanine is used as a catalyst, the rutaecarpin analogue is sy...

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Bibliographische Detailangaben
Hauptverfasser: KONG XIANGFEI, GOU TIANTIAN, WANG GUIXIA, ZHOU CHAO, ZHANG LINFENG, WANG LIANGFENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a rutaecarpin analogue as well as a preparation method and application thereof, and belongs to the field of pharmaceutical chemistry synthesis. A 4 (3H)-quinazolinone derivative is used as a substrate, iron phthalocyanine is used as a catalyst, the rutaecarpin analogue is synthesized through an intramolecular hydrogen borrowing reaction, the yield is high, and the production cost is low. When the concentration is 25 mu M and the LPS concentration is 1 mu g/mL, the NO release inhibition capacities of the compounds 1c, 1t, 1u and 1v are superior to those of an anti-inflammatory drug indometacin, and 1a, 1b and 1i are equivalent to those of indometacin; the cytotoxic effect of compounds 1c, 1t, 1u and 1v, which are relatively strong in NO release inhibition capability, on RAW264.7 cells is relatively weak; the anti-inflammatory effect is obvious, the toxicity is very low, and the pharmaceutical composition has very high medical value and wide market prospect. 本发明涉及一种吴茱萸次碱类似物及其制备方法和应用,属于药