张寅生, 曹观坤, 彭司勋, 戴德哉, 晋玲. 非甾体抗炎药4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)-胺甲基-苯酚衍生物的合成及其生物活性J. 药学学报, 1986, 21(5): 345-355.
引用本文: 张寅生, 曹观坤, 彭司勋, 戴德哉, 晋玲. 非甾体抗炎药4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)-胺甲基-苯酚衍生物的合成及其生物活性J. 药学学报, 1986, 21(5): 345-355.
ZHANG Yin-Shen, CAO Guan-Kun, PENG Si-Xun, DNI De-zai , JIN Ling, . STUDIES ON NONSTEROIDAL ANTIINFLAMMATORY DRUGS: SYNTHESIS AND BIOLOGICAL ACTIVITY OF 4-HYDROXY-3-AMINOMETHYL-DIPHENYL AND 4(2)-CYC-LOHEXYL-2(4)-AMINOMETHYL-PHENOL DERIVATIVESJ. Acta Pharmaceutica Sinica, 1986, 21(5): 345-355.
Citation: ZHANG Yin-Shen, CAO Guan-Kun, PENG Si-Xun, DNI De-zai , JIN Ling, . STUDIES ON NONSTEROIDAL ANTIINFLAMMATORY DRUGS: SYNTHESIS AND BIOLOGICAL ACTIVITY OF 4-HYDROXY-3-AMINOMETHYL-DIPHENYL AND 4(2)-CYC-LOHEXYL-2(4)-AMINOMETHYL-PHENOL DERIVATIVESJ. Acta Pharmaceutica Sinica, 1986, 21(5): 345-355.

非甾体抗炎药4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)-胺甲基-苯酚衍生物的合成及其生物活性

STUDIES ON NONSTEROIDAL ANTIINFLAMMATORY DRUGS: SYNTHESIS AND BIOLOGICAL ACTIVITY OF 4-HYDROXY-3-AMINOMETHYL-DIPHENYL AND 4(2)-CYC-LOHEXYL-2(4)-AMINOMETHYL-PHENOL DERIVATIVES

  • 摘要: 为了寻找作用强、毒副作用小的非甾体抗炎药,以取代酚类为原料,通过Mannich反应合成了26个4-羟基-3-胺甲基-联苯及4(2)-环己基-2(4)胺甲基-苯酚衍生物,对其中23个化合物进行了初步药理筛选,发现部分化合物在大鼠模型有明显的抗炎活性并有镇痛、解热作用。对其中20个化合物进行了抗着床筛选,以7.5 mg/kg剂量给予交配后的大鼠,结果均无抗着床活性。

     

    Abstract: With an attempte to search for potent nonsteroidal antiinflammatory drugs with less side-effects,twenty Six derivatives of 4-hydroxy-3-aminomethyldiphenyl and 4(2)-cyclohexyl,-2(4)-aminomethylphenol were prepared by Mannich reaction. Nineteen of the compounds were tested in rats. Some of these compounds showed significant antiinflammatory and antipyretic-analgesic activities. Antiimplanration test was also carried out on twenty of the compounds, but none was found active.

     

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