抗结核药物。第 5 部分：苯并噻二嗪 1,1-二氧化物同类物的合成与生物评价。
Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
机构信息
Division of Organic Chemistry-I, Indian Institute of Chemical Technology, Tarnaka, Hyderabad-500 607, India.
出版信息
Eur J Med Chem. 2010 Oct;45(10):4545-53. doi: 10.1016/j.ejmech.2010.07.015. Epub 2010 Jul 14.
In an effort to discover new and effective chemotherapeutic agents from this laboratory for the treatment of tuberculosis, here in we describe the synthesis and biological evaluation of a series of novel benzothiadiazine 1,1-dioxide (BTD) based congeners by using rifampicin, streptomycin; ciprofloxacin and amphotericin as positive controls. Further, to understand structural requirements for exploring the structure activity relationship of BTDs, cytotoxicity and in vivo study of recently reported potent molecule 4 (MIC = 1 microg/mL) is also discussed.
为了从本实验室发现新的、有效的抗结核化学治疗药物，我们在这里描述了一系列新型苯并噻二嗪 1,1-二氧化物（BTD）类似物的合成和生物评价，使用利福平、链霉素、环丙沙星和两性霉素作为阳性对照。此外，为了了解探索 BTDs 结构活性关系的结构要求，还讨论了最近报道的有效分子 4（MIC=1μg/mL）的细胞毒性和体内研究。
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