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[具有化疗活性的硝基化合物。第二篇通讯:硝基二苯砜(作者译)]

[Chemotherapeutically active nitro compounds. 2nd communication: Nitrodiphenyl sulfones (author's transl)].

作者信息

Winkelmann E, Raether W, Wagner W H

出版信息

Arzneimittelforschung. 1976;26(8):1543-7.

PMID:795435
Abstract

A number of new 4-nitro-4'-amino-diphenyl sulfones and related compounds were prepared and investigated as to their therapeutic activity. They showed a good systemic activity against tubercle bacilli (M. bovis, NMRI mouse) and plasmodia (P. berghei, NMRI mouse). The test results reveal that the 4-nitro-4'-amino-diphenyl sulfones possess a spectrum of activity similar to that of diamino-diphenyl sulfone (DDS). It is assumed that 4-nitro-4'-amino-diphenyl sulfones in vivo are converted into DDS derivatives by reduction. The advantages of the new compounds, however, were too insignificant as compared to DDS to justify further extensive trials.

摘要

制备了多种新型4-硝基-4'-氨基二苯砜及其相关化合物,并对其治疗活性进行了研究。它们对结核杆菌(牛分枝杆菌,NMRI小鼠)和疟原虫(伯氏疟原虫,NMRI小鼠)显示出良好的全身活性。试验结果表明,4-硝基-4'-氨基二苯砜具有与二氨基二苯砜(DDS)相似的活性谱。据推测,4-硝基-4'-氨基二苯砜在体内通过还原转化为DDS衍生物。然而,与DDS相比,新化合物的优势并不显著,不值得进一步进行广泛试验。

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