| 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 |
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| 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 |
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| 作者姓名： | 胡璧 刘维勤 |
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| 作者单位： | 中国医学科学院放射医学研究所药物室,天津;*北京医科大学药学院 |
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| 摘 要： | 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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| 关 键 词： | 对-氯苯丙炔酰胺 桂皮酰胺 桂皮酰肼 吡唑酮 抗惊作用 |
| 收稿时间： | 1985-12-18 |
STUDIES ON SYNTHESIS OF p-CHLOROPHENYLPROPIOLYLAMIDES AND ITS REACTION PRODUCTS WITH HYDRAZINE |
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| HU Bi and LIU Wei-Qin. STUDIES ON SYNTHESIS OF p-CHLOROPHENYLPROPIOLYLAMIDES AND ITS REACTION PRODUCTS WITH HYDRAZINE[J]. Acta pharmaceutica Sinica, 1986, 21(10): 787-791 |
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| Authors: | HU Bi and LIU Wei-Qin |
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| 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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| Keywords: | Cinnamamide Cinnamoyl hydrazide Pyrazolone Anticonvulsant activity p-Chlorophenylpropiolylamide |
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