Synthesis and biological evaluation of some 4-(isoxazolinyl or 1,2,4-oxadiazolyl) coumarins |
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Authors: | Demetrios N Nicolaides Konstantina C Fylaktakidou Konstantinos E Litinas Dimitra Hadjipavlou-Litina |
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Abstract: | Reaction of compound 3 with nitrile oxide 4a affords compounds 5a and 6 in 73% and 3% yield respectively, while reaction of 3 with 4b affords only compound 5b (85%). Reactions of compound 8 with the nitrile oxides 4a,b result in compounds 9a,b . The compound 10 , prepared from 1 and O-methylhydroxylamine, reacts with nitrile oxide 4b to give the oxadiazole derivative 12 . The above referred coumarins are screened for antiinflammatory activity in vivo using the carrageenin rat paw edema and in vitro through their antiproteolytic activity and their ability to inhibit β-glucuronidase and 12-Lipoxygenase. |
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