The inflammatory response is the reaction of living tissue to an injury of a foreign nature, such as infection and irritants, and occurs as part of the body's natural defence response. Compounds capable of inhibiting cyclooxygenase (COX) enzymes, especially COX-2, have great potential as anti-inflammatory agents. Herein we present the regioselective synthesis of 49 novel compounds based on the 2-pyridone nucleus. The topical anti-inflammatory activity of seventeen compounds was evaluated in mice by croton oil (CO) induced ear edema assay. Most of the compounds exhibited a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity. The most active compounds (2a and 7a) were inhibitors of COX enzymes. Compound 2a selectively inhibited the COX-2, while 7a was nonselective. Further, the compound 2a showed effective binding at the active site of COX-2 co-crystal by docking molecular study.

炎症反应是活组织对异物损伤（如感染和刺激物）的反应，并作为人体自然防御反应的一部分而发生。能够抑制环氧合酶（COX）的化合物，尤其是COX-2，具有作为消炎药的巨大潜力。本文中，我们介绍了基于2-吡啶酮核的49种新型化合物的区域选择性合成。通过巴豆油（CO）诱导的耳部水肿试验评估了17种化合物在小鼠中的局部抗炎活性。大多数化合物表现出高水平的体内抗炎活性，减少了耳部水肿和髓过氧化物酶（MPO）的活性。活性最高的化合物（2a和7a）是COX酶的抑制剂。复合2a选择性抑制COX-2，而7a非选择性。此外，通过对接分子研究，化合物2a在COX-2共晶体的活性部位显示出有效结合。