Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, India.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3721-5. doi: 10.1016/j.bmcl.2010.04.082. Epub 2010 Apr 24.
In search for a new analgesic and anti-inflammatory agent with improved potency, we designed and synthesized a series of 3,2-(4,5-dihydro-5-(4-morphilinophenyl)-1H-pyarazol-3-yl)phenols 6(a-g) and its N-phenylpyrazol-1-carbothioamide 7(a-g) by Claisan-Schmidt condensation followed by the reaction of hydrazine hydrate. All the synthesized compounds were assayed for their in vivo analgesic and anti-inflammatory activities. All the compounds synthesized showed the potential to demonstrate analgesic and anti-inflammatory activity, of particular interest compounds 6a, 6b, 6g, 7a, 7d and 7g were found comparable to Diclofenac.
为了寻找一种新的、效力更强的镇痛和抗炎药物，我们通过 Claisen-Schmidt 缩合反应以及肼水合反应设计并合成了一系列 3,2-(4,5-二氢-5-(4-吗啉基苯基)-1H-吡唑-3-基)苯酚 6(a-g)及其 N-苯并吡唑-1-碳酰硫代酰胺 7(a-g)。所有合成的化合物都进行了体内镇痛和抗炎活性测试。所有合成的化合物都显示出具有镇痛和抗炎活性的潜力，其中特别值得关注的化合物 6a、6b、6g、7a、7d 和 7g 的活性与双氯芬酸相当。
