陳世骢, 甘品珍, 錢挹芬, 胡玉琴. 血吸虫病化学治疗取代水楊酰苯胺类和笨 唑衍生物的合成J. 药学学报, 1963, 10(11): 683-687.
引用本文: 陳世骢, 甘品珍, 錢挹芬, 胡玉琴. 血吸虫病化学治疗取代水楊酰苯胺类和笨 唑衍生物的合成J. 药学学报, 1963, 10(11): 683-687.
CHEN SHIH-TSUNG, KAN PIN-CH'EN, CHEIN I-FENG AND HU Y-CHIN, . CHEMOTHERAPY OF SCHISTOSOMIASIS SYNTHESIS OF SUBSTITUTED SALICYLANILIDES AND BENZIMIDAZOLE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1963, 10(11): 683-687.
Citation: CHEN SHIH-TSUNG, KAN PIN-CH'EN, CHEIN I-FENG AND HU Y-CHIN, . CHEMOTHERAPY OF SCHISTOSOMIASIS SYNTHESIS OF SUBSTITUTED SALICYLANILIDES AND BENZIMIDAZOLE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1963, 10(11): 683-687.

血吸虫病化学治疗取代水楊酰苯胺类和笨 唑衍生物的合成

CHEMOTHERAPY OF SCHISTOSOMIASIS SYNTHESIS OF SUBSTITUTED SALICYLANILIDES AND BENZIMIDAZOLE DERIVATIVES

  • 摘要: 三十四种取代水杨酰苯胺类化合物是以取代水锡酸或取代水杨酸苯酯和取代苯胺缩合,或用取代水杨酰苯胺类经硝化而成.九种苯骈咪唑衍生物是以取代水杨酸和邻苯二胺,用多磷酸为环合剂缩合而成.所合成的化合物有几个经初步预防和治疗日本血吸虫病动物筛选试验,发现N-(5-氯水杨酰)-2′-氯-4′-硝基苯胺和N-(3,5-二氯水杨酰)-2′-氯-4′-硝基苯胺有预防作用,N-(3,5-二碘水杨酰)-2′,4′-二氯苯胺有治疗作用.

     

    Abstract: Thirty-four substituted salicylanilides were prepared by condensation of substituted salols or salicylic acids with substituted anilines, or by nitration of a substituted salicylanilide with addition of a nitro-group at the 3-position on the salicyl nucleus. Nine substituted 2(o-hydroxy-phenyl)-benzimidazoles were prepared by condensation of substituted salicylic acids with o-phenylenediamine in presence of polyphosphoric acid at temperature between 120—250℃ for four hours. Some of the resulted compounds were screened in mice against schistosomiasis japonica. The results indicated that two compounds, 5, 2'-dichloro-4'-nitro-salicylanilide and 3, 5, 2' - trichloro-4'-nitro - salicylanilide showed chemoprophylactic activity, and the compound 3,5-diiodo-2',4'-dichloro-salicylanilide possessed chemotherapeutic activity.

     

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