Pyrimidine Derivatives and Related Compounds. XX. Synthesis and Analgetic and Antiinflammatory Activities of 1,3-Disubstituted 5-Dialkylaminomethyluracil Derivatives
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As a part of our studies on the structure-activity relationship of 1,3-disubstituted 5-dialkylamino-6-methyluracil derivatives, we have synthesized 1,3-disubstituted 5-dialkylaminomethyl-6-methyluracils (B). In the synthesis, 1,3-disubstituted 5-cyano-uracils (1-6) were hydrogenated with Raney-cobalt followed by methylation to give the 5-dimethylaminomethyluracil compounds (16-20). The Mannich reaction of 1,3-disubstituted uracils (23-26,33) did not proceed, but halogenomethylation of them and subsequent amination gave the 5-dialkylaminomethyl compounds (20,34-41). As to their pharmacological activities, analgetic, antipyretic and antiinflammatory activities and acute toxicity were tested. The compounds (B) showed only antiinflammatory activity.
- 公益社団法人日本薬学会の論文
- 1974-05-25
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