Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysuru, Karnataka, India.
Department of Biochemistry, Farooqia Dental College, Mysuru, Karnataka, India.
Bioorg Chem. 2019 Nov;92:103220. doi: 10.1016/j.bioorg.2019.103220. Epub 2019 Aug 26.
The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body's response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This reaction is catalyzed by cyclooxygenase, a membrane associated enzyme occurring in two isoforms, COX-1 and COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) act by inhibiting the activity of COX. In view of this, a series of novel benzophenones conjugated with oxadiazole sulphur bridge pyrazole moiety 8a-l were designed, synthesized, characterized and subsequently evaluated for anti-inflammatory and analgesic property. The investigation of novel analogues 8a-l for potential anti-inflammatory activity showed high levels of COX-1 and COX-2 inhibitory activity. Among the series, compound 8i with electron withdrawing fluoro group at the para position of the benzoyl ring of benzophenone was characterized by highest IC values for both COX-1 and COX-2 inhibition, which is comparable to the standard drug. Further, molecular docking studies have been performed for the potent compound.
前列腺素（PG）是一组具有多种激素样作用的生理活性脂质化合物，是机体对疼痛和炎症反应的重要介质，由细胞膜中存在的必需脂肪酸形成。这一反应由环氧化酶催化，环氧化酶是一种膜相关酶，存在两种同工型，COX-1 和 COX-2。非甾体抗炎药（NSAIDs）通过抑制 COX 的活性起作用。有鉴于此，设计、合成、表征了一系列与恶二唑硫桥吡唑部分连接的新型二苯甲酮 8a-l，并对其抗炎和镇痛特性进行了评估。新型类似物 8a-l 的抗炎活性研究显示出对 COX-1 和 COX-2 的高抑制活性。在该系列中，苯甲酰苯酮苯环对位带有吸电子氟基团的化合物 8i 对 COX-1 和 COX-2 的抑制作用最强，与标准药物相当。此外，还对有效化合物进行了分子对接研究。
