Post Graduate & Research Centre, Department of Chemistry, MES Abasaheb Garware College, Pune, India.
Bioorg Med Chem Lett. 2013 Feb 1;23(3):711-4. doi: 10.1016/j.bmcl.2012.11.097. Epub 2012 Dec 3.
One pot synthesis of 3-Aracylphthalide was accomplished in good yield by reacting 2-carboxy benzaldehyde with various aromatic methyl ketones in presence of methane sulphonic acid. Various phthalides thus obtained were characterized with spectral techniques. These phthalides were subjected to in vitro antitubercular screening against Mycobacterium tuberculosis H37Ra (MTB) by using XRMA protocol. Among the phthalides screened, four exhibited half maximal inhibitory concentration (IC(50)) in the range of 0.81-1.24 μg/ml thereby providing potential lead compounds for future drug discovery studies.
一锅法合成 3-取代苯酞，在甲烷磺酸存在下，用 2-羧酸苯甲醛与各种芳香族甲基酮反应，高产率得到 3-取代苯酞。所得各种苯酞均用光谱技术进行了表征。用 XRMA 方案，根据体外抗结核筛选方法，对这些苯酞进行了对结核分枝杆菌 H37Ra（MTB）的活性筛选。在所筛选的苯酞中，有 4 种的半最大抑制浓度（IC50）在 0.81-1.24 μg/ml 范围内，从而为未来的药物发现研究提供了潜在的先导化合物。
