1,5-二芳基咪唑类化合物对脂多糖诱导的 RAW 264.7 细胞中环氧化酶-2 催化的 PGE2 生成具有强抑制活性。
1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells.
机构信息
College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Jul 15;20(14):4035-7. doi: 10.1016/j.bmcl.2010.05.092. Epub 2010 May 27.
A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE(2) production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the position of the 4-methylsulfonylphenyl group. The 1,5-diarylimidazoles with a halogen atom (3c-3h, 3n-3p) gave mostly excellent inhibitory activities regardless of the position and species of the halogen atom. Whereas the 1,5-diarylimidazoles with two fluorine atoms (3k, 3l, 3r, 3s) showed rather reduced inhibitory activities.
一系列带有 4-甲基磺酰基苯基的 1,5-二芳基咪唑被制备出来，并评价了它们对 COX-2 催化的 LPS 诱导的 RAW 264.7 细胞中 PGE(2)产生的抑制活性。大多数合成的 1,5-二芳基咪唑都表现出很强的抑制活性，而与 4-甲基磺酰基苯基的位置无关。带有卤素原子（3c-3h、3n-3p）的 1,5-二芳基咪唑无论卤素原子的位置和种类都表现出极好的抑制活性。而带有两个氟原子（3k、3l、3r、3s）的 1,5-二芳基咪唑的抑制活性则降低了。
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