胡璧, 刘维勤. 对-氯苯丙炔酰胺类化合物的合成及其与肼反应产物的研究J. 药学学报, 1986, 21(10): 787-791.
引用本文: 胡璧, 刘维勤. 对-氯苯丙炔酰胺类化合物的合成及其与肼反应产物的研究J. 药学学报, 1986, 21(10): 787-791.
HU Bi, LIU Wei-Qin. STUDIES ON SYNTHESIS OF p-CHLOROPHENYLPROPIOLYLAMIDES AND ITS REACTION PRODUCTS WITH HYDRAZINEJ. Acta Pharmaceutica Sinica, 1986, 21(10): 787-791.
Citation: HU Bi, LIU Wei-Qin. STUDIES ON SYNTHESIS OF p-CHLOROPHENYLPROPIOLYLAMIDES AND ITS REACTION PRODUCTS WITH HYDRAZINEJ. Acta Pharmaceutica Sinica, 1986, 21(10): 787-791.

对-氯苯丙炔酰胺类化合物的合成及其与肼反应产物的研究

STUDIES ON SYNTHESIS OF p-CHLOROPHENYLPROPIOLYLAMIDES AND ITS REACTION PRODUCTS WITH HYDRAZINE

  • Abstract: Synthesis of p-chlorophenylpropiolylamides and itsreaction produets with hydrazine hydrate were studied. It was found that the reaction products varied with the different Substituent groups in the amidel When the substituent group was isopropyl or sec-butyl group, p-chloro-β-hydrazino-cinnamamides (Ⅱ) were obtained. Under similar reaction conditions, when the substituent, group was n-propyl, n-butyl or diethyl group, cyclization reaction occurred and the reaction product was 3-(p-chlorophenyl)-pyrazol-5-one (Ⅲ). All the compounds were tested in mice for anticonvulsant activity. Prelimary data showed that p-chlorophenyl-propiolyl-sec-butylamide (I4) and p-chlorophenyl-propiolyl-n-propylamide (I1) exhibited moderate anticonvulsant activity. The ED50 was 54.5(34.4~86.4), and 56.1(31.6~99.6) mg/kg respectively. The compounds of p-chloro-β-hydrazino-cinnamamide (Ⅱ)and 3-(p-chlorophenyl)-pyrazol-5-one (Ⅲ) showed no significant effect on antieonvulsant activity. p-Chloro-cinnamoyl-hydrazide (Ⅳ) provided good anticonvulsant activity.

     

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