Department of Chemistry, Vinyakrao Patil Mahavidyala Vaijapur, Aurangabad, MS 423701, India.
Bioorg Med Chem Lett. 2011 Nov 1;21(21):6527-32. doi: 10.1016/j.bmcl.2011.08.061. Epub 2011 Sep 10.
A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema method. Diclofenac sodium was used as a standard drug for comparison. Out of the 30 compounds tested, compound 19a, 19b, 25a, 25b exhibited significant anti-inflammatory activity. Selected compounds were also screened for in vitro COX-2 inhibition assay and analgesic activity in the acetic acid induced writhing model.
为了获得具有潜在抗炎活性的新化合物，设计并合成了一系列 4,5-二氢-1,5-二芳基-1H-吡唑-3-取代的杂环唑。采用角叉菜胶诱导大鼠足肿胀法筛选标题化合物的体内抗炎活性。双氯芬酸钠用作比较标准药物。在所测试的 30 种化合物中，化合物 19a、19b、25a、25b 表现出显著的抗炎活性。还对选定的化合物进行了体外 COX-2 抑制试验和醋酸诱导扭体模型中的镇痛活性筛选。
