クマリン誘導体の合成研究 (第8報)

クマリン-3-カルボン酸誘導体の鎮静催眠作用について

抄録

Soporific and sedative actions and toxicity of 25 kinds of coumarin-3-carboxylic acid derivatives were examined in mice and the results obtained are listed in the accompanying Tables and Figures.
1) Esters possess some efficacy and the effect is stronger in alkyl esters than in phenyl esters.
2) In alkly esters, the activity became weaker with the increase in the size of the alkyl group and in the same alkyl group, the normal chain was weaker than the iso chain.
3) Compounds of -CONHR type where the R is an aromatic ring or ureido compounds were ineffective and devoid of toxicity.
4) Substitution of coumarin ring in the 6-position with nitro, amino, or acetylamino group caused loss of efficacy and toxicity.
5) The same substitution in the 7-position of the coumarin ring also caused loss of the sedative and soporific activities but not of toxicity, which appeared gradually over a few days.