アミノアルコール誘導体の研究(第3報)ジヘテロ異項環化合物の合成および薬理作用

概要

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In order to investigate the relation between chemical structure and the pharmacological activities, 67 new compounds belonging to cyclic compounds containing two hetero atoms which were derived from 1-alkylamino-3-dialkylamino-2-propanol were synthesized. These compounds were examined for local anesthetic activity, antispasmodic activity, inhibitory activity on writhing syndrome produced by acetic acid, and analgesic activity on pain produced by hot plate. Several of them showed three or four times longer duration of infiltration anesthesia than lidocaine. 5-Dipropylaminomethyl-3-methyl-2-oxazolidone hydrobromide (C_3), 5-piperidinomethyl-3-propyl-2-oxazolidone hydrobromide (C_<24>), 6-piperidinomethyl-4-phenyl-2,3-morpholinedione hydrobromide (D_<20>), 2-dibutylaminomethyl-4-methylperhydro-1,4-oxazepin-5,7-dione hydro bromide (E_4) and 2-piperidinomethyl-4-phenylperhydro-1,4-oxazepin-5,7-dione hydrobromide (E_<21>) were proved to have antispasmodic activity at the concentration from 7.5-1.0×10^<-6> g/ml. Several of the compounds showed as potent an analgesic activity as pyrabital. Cyclic compounds containing two hetero atoms had lower toxicity than aminoalcohols. In general, the pharmacological activity decreased in the order of 2-oxazolidone (C), perhydro-1,4-oxazepin-5,7-dione (E), and 2,3-morpholinedione (D).
公益社団法人日本薬学会の論文
1974-04-25