Department of Oncology, University of Alberta, Edmonton, Alberta, Canada.
Bioorg Med Chem Lett. 2012 Mar 15;22(6):2235-8. doi: 10.1016/j.bmcl.2012.01.093. Epub 2012 Feb 2.
A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles contained a methylsulfonyl or sulfonamide group as COX-2 pharmacophore displayed only low inhibitory potency towards COX-2. Most potent compounds showed IC(50) values of 6 and 7 μM for COX-2. All compounds showed IC(50) values greater 100 μM for COX-1 inhibition.
通过四氯硅烷/叠氮化钠处理各种二芳基酰胺，制备了一系列新型 5-取代 1H-四唑类环氧化酶-2（COX-2）抑制剂。所有化合物均在体外环氧化酶（COX）测定中进行测试，以确定 COX-1 和 COX-2 的抑制效力和选择性。四唑类化合物含有甲磺酰基或磺酰胺基作为 COX-2 药效团，对 COX-2 仅显示出低抑制效力。最有效的化合物对 COX-2 的 IC（50）值为 6 和 7 μM。所有化合物对 COX-1 抑制的 IC（50）值均大于 100 μM。
