Sriram Dharmarajan, Yogeeswari Perumal, Thirumurugan Rathinasabapathy
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.
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。
