Background: Quinolines are an important class of heterocyclic compounds possessing a wide range of biological activities. Previously, we had identified Schiff bases of quinoline as potential anti-inflammatory agents, thus the current work is the continuation of our previous study.

Objective: In the current study, 3-, 5-, and 8-sulfonamide and 8-sulfonate derivatives of quinoline (1-50) were synthesized and their anti-inflammatory potential was evaluated. These synthetic analogs were evaluated for their anti-inflammatory activity via ROS (Reactive oxygen species) inhibitory effect produced from phagocytes from human whole blood.

Methods: The sulfonamide and sulfonate derivatives of quinoline were synthesized via treating 5-, 3-, 8-amino, and 8-hydroxy quinolines with different substituted sulfonyl chlorides in pyridine. The synthetic molecules were characterized using various spectroscopic techniques and screened for their anti-inflammatory potential.

Results: Among the synthetic derivatives 1-50, six compounds showed good to moderate antiinflammatory activity. Compounds 47 (IC₅₀ = 2.9 ± 0.5 μg/mL), 36 (IC₅₀ = 3.2 ± 0.2 μg/mL), and 24 (IC₅₀ = 6.7 ± 0.3 μg/mL) exhibited enhanced activity as compared to the standard ibuprofen (IC₅₀ = 11.2 ± 1.9 μg/mL). Compounds 20 (IC₅₀ = 25.5 ± 0.7 μg/mL), 50 (IC₅₀ = 42.9 ± 5.6 μg/mL), and 8 (IC₅₀ = 53.9 ± 3.1 μg/mL) were moderately active, however, rest of the compounds were found to be inactive.

Conclusion: The sulfonamide and sulfonate derivatives of quinoline were found to have promising anti-inflammatory activity. Further studies on the modification of these molecules may lead to the discovery of new and potential anti-inflammatory agents.

背景：喹啉是一类重要的杂环化合物，具有广泛的生物活性。以前，我们已经确定喹啉的席夫碱为潜在的抗炎药，因此当前的工作是我们先前研究的延续。

目的：在本研究中，合成了喹啉（1-50）的3-，5-和8-磺酰胺和8-磺酸酯衍生物，并评估了它们的抗炎潜力。通过人全血吞噬细胞产生的ROS（活性氧）抑制作用评估了这些合成类似物的抗炎活性。

方法：通过在吡啶中用不同的取代磺酰氯处理5-，3-，8-氨基和8-羟基喹啉，合成喹啉的磺酰胺和磺酸盐衍生物。使用各种光谱技术对合成分子进行表征，并筛选其抗炎潜力。

结果：在合成衍生物1-50中，六种化合物显示出良好到中等的抗炎活性。化合物47（IC ₅₀ = 2.9±0.5μg/ mL），36（IC ₅₀ = 3.2±0.2μg/ mL）和24（IC ₅₀ = 6.7±0.3μg/ mL）与标准布洛芬（ IC ₅₀ = 11.2±1.9μg/ mL）。化合物20（IC ₅₀ = 25.5±0.7μg/ mL），化合物50（IC ₅₀ = 42.9±5.6μg/ mL）和8（IC ₅₀ = 53.9±3.1μg/ mL）具有中等活性，但是其余化合物被发现处于非活动状态。

结论：喹啉的磺酰胺和磺酸盐衍生物具有良好的抗炎活性。对这些分子的修饰的进一步研究可能导致发现新的和潜在的抗炎剂。