Background: A novel series of 2-[(2-{[2-(furan-2-yl) quinolin-4-yl] carbonyl} hydrazinyl) carbonyl] benzoic acid, -4-oxobut-2-enoic acid and -4-oxobutanoic acids were synthesized and screened for in vitro antitubercular activity.

Objectives: In the present investigation, we describe the synthesis and biological screening of furan C-2 quinoline coupled diamides for antitubercular activity.

Methods: The mycobacterium tuberculai testing was carried out by MABA method and molecular docking studies were done by open-source molecular docking program, Autovina, using Pyrx 0.8 interface.

Results: The results revealed that the compounds inhibited the growth of H37Rv strain at concentrations as low as 1.6 to 12 µg/ml. Molecular binding of furan, quinoline and diamide (FQD) derivatives on five targets was good and these compounds fit very well within the binding domain of the target protein.

Conclusion: The synthesized FQD derivatives exhibited moderate to good inhibition activity especially compounds 5f, 5b and 8a exhibited very good inhibition activity due to the presence of three different scaffolds, such as INH, phenyl ketobutyric acid and fluoroquinolines. Hybridized molecules might have multiple modes of action / inhibit more than one tubercular target and could pave way for novel drug discovery in the field of tuberculosis.

背景：2-[（（2-{[2-（呋喃-2-基）喹啉-4-基]羰基}肼基）羰基]苯甲酸，-4-氧代丁-2-烯酸和-4的新系列合成-氧代丁酸并筛选其体外抗结核活性。

目的：在本研究中，我们描述了呋喃C-2喹啉偶联的二酰胺类抗结核活性的合成和生物学筛选。

方法：采用MABA法进行结核分枝杆菌检测，并使用Pyrx 0.8接口通过开源分子对接程序Autovina进行分子对接研究。

结果：结果表明，该化合物以低至1.6至12 µg / ml的浓度抑制H37Rv菌株的生长。呋喃，喹啉和二酰胺（FQD）衍生物在五个靶标上的分子结合良好，这些化合物非常适合目标蛋白的结合域。

结论：合成的FQD衍生物具有中等至良好的抑制活性，尤其是化合物5f，5b和8a由于存在3种不同的支架（如INH，苯基酮丁酸和氟喹啉）而具有非常好的抑制活性。杂交分子可能具有多种作用模式/抑制一个以上的结核靶标，并可能为结核病领域的新药发现铺平道路。