Biological antirheumatic activity

Source Siegesbeckia oreintalis. Biological activity Antirheumatic. 

The whole plant of Incarvillea sinensis is used in traditional Chinese medicine as an antirheumatic and analgesic (88). Examination of the alkaloid content led to a number of new monoterpene pyridine alkaloids discussed earlier (see Section II.A.20-22). Biological evaluation of the isolates indicated that incarvillateine (34) at 10 mg/kg i.p. inhibited both the first and second stages of formalin-induced pain and reduced spontaneous motor activity. At lower doses (1-5 mg/kg), the analgesic activity was maintained without sedative activity (88). 

Among the isoxazoles, many biologically active compounds are found. Some of them are important as drugs or biocides, e.g. the long-acting sulfonamide sulfamethoxazole 10, the anti-inflammatory isoxi-cam 11, the antiarthritic and antirheumatic leflunomide 12 and the fungicide 3-hydroxy-5-methylisoxazole. 

An efficient and general method to prepare diverse P-ketoesters linked to a solid support was developed by Tietze et al. using readily available acid chlorides 259 and haloalkanes as building blocks. The obtained polymer-bound 1,3-dicarbonyl compounds served as substrates toward the preparation of a library of substituted pyrazolones, which are well known for their widespread biological activity as analgesics, antipyretics, antiphlogistics, antirheumatics, antiarthritics and... 

BIOLOGICAL ACTIVITY Used as antiinflammatory, antibacterial and antirheumatism agent in China [1602]. 

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