Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
Pyrimidine Derivatives and Related Compounds. XX. Synthesis and Analgetic and Antiinflammatory Activities of 1, 3-Disubstituted 5-Dialkylaminomethyluracil Derivatives
SHIGEO SENDAKOSAKU HIROTAJIYOJI NOTANI
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Volume 22 (1974) Issue 5 Pages 1179-1185

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Abstract

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.

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