化学学报 ›› 1955, Vol. 21 ›› Issue (2): 115-121. 上一篇    下一篇

论文

4-氨基-2-烷磺醯苯甲酸的合成及其对于结核桿菌的抑制性能

施嘉锺, 嚴燊和   

  1. 上海第一医学院有机化学教研组
  • 投稿日期:1955-01-09 发布日期:2013-06-04

SYNTHESIS OF 4-AMINO-2-ALKYLSULFONYL BENZOIC ACIDS AND THEIR TUBERCULOSTATIC ACTIVITIES

SHIH CHIA-CHUNG, YEN HSIN-HO   

  1. The First Medical College of Shanghai
  • Received:1955-01-09 Published:2013-06-04

對-氨基柳酸為現在常用的一種結核病治療藥劑。我們將其中的羥基代以-SO2R,希望能增強其抑制結核桿菌的性能。我們合成了4-氨基-2-甲磺醯苯甲酸,4-氨基-2-乙磺醯苯甲酸和4-氨基-2-正丙磺醯苯甲酸三種新的化合物。在試管中試驗的結果,除最後一種化合物能在千分之一濃度的溶液中具抑制結核桿菌的性能外,其餘兩種化合物抑制結核桿菌的性能則是更低。我們在製備上述三種化合物時,曾附带合成另外五種新的化合物。

Three new 4-amino-2-alkylsulfonyl benzoi:: acids, namely, 4-amino-2-methylsulfonyl benzoic acid, 4-amino-2-ethylsulfonyl benzoic acid and 4-amino-2-n-propylsulfonyl benzoic acid, have been studied for in vitro in human tuberculosis, hoping that they would surpass the p-amino- salicylic acid in activity. Contrary to our expectations, however, these new compounds have been found to be far less active than the p-amino-salicylic acid itself. The 4-amino-2-n-propyl-sulfonyl benzoic acid possesses an activity in the order of 10-3 in concentration, while the other two compounds require still higher concentrations.