某些芳基氨基脲衍生物的抗结核活性
Antituberculous activity of some aryl semicarbazone derivatives.
作者信息
Sriram Dharmarajan, Yogeeswari Perumal, Thirumurugan Rathinasabapathy
机构信息
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.
出版信息
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3923-4. doi: 10.1016/j.bmcl.2004.05.060.
During the course of our work on the synthesis and screening of new drugs for tuberculosis, we have identified N1-(4-acetamido phenyl)-N4-(2-nitro benzylidene) semicarbazone (1b), which inhibited in vitro Mycobacterium tuberculosis H(37)Rv; 100% inhibition at 1.56 microg/mL. This paper is first of its kind in which aryl semicarbazones are reported to possess antimycobacterials potency greater than p-aminosalicylic acid, ethionamide, ethambutol, ciprofloxacin and kanamycin.
在我们开展结核病新药合成与筛选工作的过程中，我们鉴定出了N1-(4-乙酰氨基苯基)-N4-(2-硝基亚苄基)氨基脲（1b），它在体外对结核分枝杆菌H(37)Rv具有抑制作用；在浓度为1.56微克/毫升时抑制率达100%。本文首次报道了芳基氨基脲具有比对氨基水杨酸、乙硫异烟胺、乙胺丁醇、环丙沙星和卡那霉素更强的抗分枝杆菌效力。
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