Phospholipase A₂ (PLA₂) is a well‐known drug target for the treatment of inflammation‐related diseases. In this study, we reported the synthesis and biological screening of a series of new carboxamides bearing sulfonamide functionality for PLA₂ inhibitory potency and 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) free radical scavenging activity. Also, computational technique was employed to characterize the binding poses of top‐ranking derivatives. The biological assay shows that all the compounds inhibited the enzyme at percentage inhibition ranging from 5.3 to 66.4 %, while only six compounds inhibited more than 60.0 % of PLA₂ activity. The six derivatives also scavenge more than 60 % of the free radical which indicates they are both potential anti‐inflammatory and anti‐oxidant candidates. Analysis of the compounds’ theoretical binding poses reveals unique binding interactions exploitable in developing enhanced PLA₂ inhibitors.

中文翻译：

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带有磺酰胺功能的羧酰胺作为潜在的新型磷脂酶A2抑制剂

磷脂酶A ₂（PLA ₂）是治疗炎症相关疾病的知名药物靶标。在这项研究中，我们报道了一系列具有磺酰胺功能的新型羧酰胺的合成和生物学筛选，这些酰胺具有PLA ₂抑制能力和2,2-二苯基-1-吡啶并肼基（DPPH）清除自由基的活性。此外，还使用计算技术来表征排名靠前的导数的绑定姿势。生物测定显示，所有化合物抑制在抑制百分比范围从5.3至66.4％的酶，而只有六个化合物抑制PLA超过60.0％₂活动。这六种衍生物还清除了60％以上的自由基，这表明它们都是潜在的抗炎和抗氧化剂的候选者。对化合物理论结合态的分析揭示了开发增强的PLA ₂抑制剂可利用的独特结合相互作用。