Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, 14801-902 Araraquara, SP, Brazil.
Eur J Med Chem. 2010 May;45(5):1898-905. doi: 10.1016/j.ejmech.2010.01.028. Epub 2010 Jan 28.
The aim of this study was to identify a candidate drug for the development of anti-tuberculosis therapy from previously synthesized compounds based on the thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones compounds. The minimal inhibitory concentration (MIC) of these compounds against Mycobacterium tuberculosis was determined. Their in vitro cytotoxicity to J774 cells (IC50) was determined to establish a selectivity index (SI) (SI=IC50/MIC). The best compounds were the thiosemicarbazones (2, 3 and 4) and the hydrazide/hydrazones (14, 15, 16 and 18). The results are comparable to or better than those of "first line" or "second line" drugs commonly used to treat TB, suggesting these compounds as anti-TB drug candidates.
本研究旨在从先前合成的基于硫代缩氨基脲、缩氨基硫脲、二硫代氨基甲酸盐和酰肼/腙化合物的化合物中，寻找一种候选药物用于开发抗结核疗法。测定了这些化合物对结核分枝杆菌的最小抑菌浓度（MIC）。测定了它们对 J774 细胞的体外细胞毒性（IC50），以建立选择性指数（SI）（SI=IC50/MIC）。最好的化合物是硫代缩氨基脲（2、3 和 4）和酰肼/腙（14、15、16 和 18）。结果与通常用于治疗结核病的“一线”或“二线”药物相当或更好，表明这些化合物是抗结核药物的候选药物。
