A series of ethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-a]quinoline-3-carboxylates 4a-f and dimethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-a]quinoline-2,3-dicarboxylates 4g-k have been synthesized and evaluated for their anti-tubercular (TB) activities against H37Rv (American Type Culture Collection (ATCC) strain 25177) and multidrug-resistant (MDR) strains of Mycobacterium tuberculosis by resazurin microplate assay (REMA). Molecular target identification for these compounds was also carried out by a computational approach. All test compounds exhibited anti-tuberculosis (TB) activity in the range of 8-128 µg/mL against H37Rv. The test compound dimethyl-1-(4-fluorobenzoyl)-5-methylpyrrolo[1,2-a]quinoline-2,3-dicarboxylate 4j emerged as the most promising anti-TB agent against H37Rv and multidrug-resistant strains of Mycobacterium tuberculosis at 8 and 16 µg/mL, respectively. In silico evaluation of pharmacokinetic properties indicated overall drug-likeness for most of the compounds. Docking studies were also carried out to investigate the binding affinities as well as interactions of these compounds with the target proteins.

中文翻译：

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吡咯并[1,2-a]喹啉衍生物的细胞毒性和抗分枝杆菌特性：分子靶标鉴定和分子对接研究。

一系列1-（取代的苯甲酰基）-5-甲基吡咯并[1,2-a]喹啉-3-羧酸乙酯4a-f和1-（取代的苯甲酰基）-5-甲基吡咯并[1,2-a]喹啉-二甲基已合成2,3-二羧酸4g-k，并通过刃天青微孔板检测评估了其对H37Rv（美国典型培养物保藏中心（ATCC）菌株25177）和结核分枝杆菌的多药耐药（MDR）菌株的抗结核（TB）活性。 （REMA）。这些化合物的分子靶标鉴定也通过计算方法进行。所有测试化合物针对H37Rv的抗结核（TB）活性范围为8-128 µg / mL。测试化合物二甲基-1-（4-氟苯甲酰基）-5-甲基吡咯并[1,2-a]喹啉-2，3-二羧酸盐4j分别以8 µg / mL和16 µg / mL的浓度成为抗H37Rv和结核分枝杆菌多药耐药菌株的最有希望的抗结核药物。在计算机上对药代动力学特性的评估表明大多数化合物的总体药物相似性。还进行了对接研究以研究这些化合物与靶蛋白的结合亲和力以及相互作用。