Chavan Hemant V, Adsul Laxman K, Kotmale Amol S, Dhakane Valmik D, Thakare Vishnu N, Bandgar Babasaheb P
Department of Organic Chemistry, Ratnagiri Sub-Centre, University of Mumbai , Ratnagiri, Maharashtra , India and.
J Enzyme Inhib Med Chem. 2015 Feb;30(1):22-31. doi: 10.3109/14756366.2013.873037. Epub 2014 Mar 25.
Abstract A series of novel pyrazole-based chalcones have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxyphenyl)-1H-pyrazole (6). The structures of regioisomers 6 and 7 were determined by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds were tested for their inhibitory activity against COX-1 and COX-2 using an in vitro cyclooxygenase (COX) inhibition assay. Moreover, they were investigated in vivo for their anti-inflammatory activities using carrageenan-induced rat paw edema model for acute inflammation and cotton pellet-induced granuloma model for chronic inflammation. All the synthesized compounds showed potential to demonstrate anti-inflammatory activities, of particular interest compounds 10i, 10e, 10f, and 10h were found to be potent anti-inflammatory agents.
摘要 设计并合成了一系列基于吡唑的新型查耳酮，其由1-甲基-5-(2,4,6-三甲氧基苯基)-1H-吡唑(6)合成。通过二维(1)H-(1)H COSY、(1)H-(13)C HSQC和(1)H-(13)C HMBC实验确定了区域异构体6和7的结构。使用体外环氧化酶(COX)抑制试验测试了新合成化合物对COX-1和COX-2的抑制活性。此外，使用角叉菜胶诱导的大鼠足爪水肿模型用于急性炎症，棉球诱导的肉芽肿模型用于慢性炎症，在体内研究了它们的抗炎活性。所有合成化合物均显示出具有抗炎活性的潜力，特别值得关注的是化合物10i、10e、10f和10h被发现是有效的抗炎剂。
