Synthesis and amelioration of inflammatory paw edema by novel benzophenone appended oxadiazole derivatives by exhibiting cyclooxygenase-2 antagonist activity
作者:Naveen Puttaswamy、Vikas H. Malojiao、Yasser Hussein Eissa Mohammed、Ankith Sherapura、B.T. Prabhakar、Shaukath Ara Khanum
DOI:10.1016/j.biopha.2018.04.167
日期:2018.7
Ten new 2(4-hydroxy-3-benzoyl) benzamide-5-phenyl-1,3,4-oxadiazole derivatives () were synthesized by coupling 3-benzoyl-4-hydroxybenzoic acid ( with 2-amino-5-phenyl-1,3,4-oxadiazoles (). The structures of these compounds were confirmed by IR, H, C NMR, and mass spectra, and also by elemental analyses. The anti-inflammatory activity of the compounds were investigated by screening them against human
通过将3-苯甲酰基-4-羟基苯甲酸(5)与2-氨基偶联,合成了十个新的2(4-羟基-3-苯甲酰基)苯甲酰胺-5-苯基-1,3,4-恶二唑衍生物(10a-j)。 -5-苯基-1,3,4-恶二唑(9a-j)。这些化合物的结构通过IR,1 H,13 C NMR和质谱以及元素分析确认。通过体外筛选化合物对抗人红细胞(HRBC)来研究化合物10a-j的抗炎活性。结果表明,在该系列中,具有羟基取代基的化合物10j,特别是在与恶二唑环的第5个碳原子连接的苯环的邻位上,与对照相比具有显着的膜稳定活性。进一步,进行了体内鸡绒膜尿囊膜(CAM)和大鼠角膜抗血管生成测定,以评估化合物10j对内皮细胞迁移的影响。这证实了化合物10j抑制内皮细胞的增殖。抗炎研究发现了角叉菜胶诱发的大鼠后爪水肿的改善。进一步的体内和计算机模拟方法揭示了炎症标记酶环氧合酶2(Cox-2)和髓过氧化物酶(MPO)的抑制作用。研究报告说,