Active site molecular modelling of xanthine oxidase inhibitors with antiinflammatory activity
✍ Scribed by Gerd Folkers; Hans-Dieter Höltje
- Publisher
- Elsevier Science
- Year
- 1985
- Tongue
- English
- Weight
- 598 KB
- Volume
- 3
- Category
- Article
- ISSN
- 0263-7855
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## ~ ~~ Phase-transfer alkylation of 2,4-dimethoxy-7H-pyrrolo[2,3-d]pyrimidine (2) with ethyl 3-bromopropionate leads regioselectively to ethyl 2,3-dimethoxy-7H-pyrrolo(2,3-d]pyrimidine-7-propionate (3a). After saponification and ether cleavage, the functionalised 7-deazaxanthine 4b was obtained.
Treatment of rabbit synovial fibroblasts with active oxygen (AO) released by xanthine/xanthine oxidase resulted in an induction of procollagenase in these cells in concentrations ranging from 12.5 micrograms/ml xanthine plus 0.0025 U/ml xanthine oxidase to 50 micrograms/ml xanthine plus 0.01 U/ml xa