Novel arylpiperazine-1,2-benzothiazine derivatives have been designed and synthesized as potential anti-inflammatory agents. Their structure and properties have been studied using spectroscopic techniques (¹H NMR, ¹³C NMR, FT-IR), MS, elemental analyses, and single-crystal X-ray diffraction (SCXRD, for compound 7b). This study aimed to evaluate the inhibitory activity of new derivatives against both cyclooxygenase isoforms COX-1 and COX-2 due to the similarity of new compounds to oxicams drugs from the NSAIDs group. All new compounds were divided into two series – A and B – with a different linker between thiazine and piperazines nitrogens. Series A included the three-carbon aliphatic linker and series B – two-carbon with a carbonyl group. According to in vitro and molecular docking studies all new compounds exhibited cyclooxygenase inhibitory activity. The series of A compounds included COX-1 inhibitors only. In contrast, the B series showed inhibition of both COX-1 and COX-2, which suggested the importance of the acetoxy linker for COX-2 inhibition. Moreover, the most selective compound 7b, towards COX-2, was non-toxic for the normal human cell line (in concentration of 10 µM) comparable to reference drug meloxicam. Additionally, investigation of influence on model membranes confirmed the ability of the compound 7b to penetrate lipid bilayers which seemed to be important to the influence with membrane protein - cyclooxygenase.

新型芳基哌嗪-1,2-苯并噻嗪衍生物已被设计和合成为潜在的抗炎剂。已经使用光谱技术（¹ H NMR、¹³ C NMR、FT-IR）、MS、元素分析和单晶 X 射线衍射（SCXRD，对于化合物7b）研究了它们的结构和性质。由于新化合物与来自 NSAIDs 组的 oxicams 药物的相似性，本研究旨在评估新衍生物对环加氧酶同种型 COX-1 和 COX-2 的抑制活性。所有新的化合物，分别分为两大系列-甲和乙-与噻嗪和哌嗪氮之间具有不同的连接体。A系列包括三碳脂肪族接头和B系列- 带有羰基的两碳。根据体外和分子对接研究，所有新化合物都表现出环氧合酶抑制活性。A系列化合物仅包括COX-1抑制剂。相比之下，B系列显示出对 COX-1 和 COX-2 的抑制，这表明乙酰氧基接头对 COX-2 抑制的重要性。此外，对 COX-2最具选择性的化合物7b对正常人细胞系（浓度为 10 µM）无毒，与参考药物美洛昔康相当。此外，对模型膜影响的研究证实了化合物7b的能力 穿透脂质双层，这似​​乎对膜蛋白 - 环氧合酶的影响很重要。